International Journal of Applied Pharmaceutics

THE DEVELOPMENT AND VALIDATION OF ANALYTICAL METHOD FOR EVALUATING GALLIC ACID IN ETHYL ACETATE FRACTION (EAF) OF SNEDDS FORMULATION: QUANTITATIVE ANALYSIS WITH IN VITRO ASSAY

2023-11-08T10:51:57+0530

Objective: This study aimed to develop a simple, accurate, precise, sensitive, robust, and stable analytical method for the evaluation of gallic acid in Self-Nanoemulsifying Drug Delivery System (SNEDDS) incorporating ethyl acetate fraction (EAF) of Melastoma malabathricum leaves in combination with Gentamicin.

Methods: Validation process followed ICH guidelines and applied a reverse phase HPLC method with a mobile phase of acetonitrile-phosphoric buffer at pH 3.03 (20:80 v/v). The stationary phase consisted of a VP-ODS shim-pack C-18 column (250x4.6 mm) with a flow rate of 0.2 ml/min and detection at 263 nm using an Ultraviolet detector. Additionally, antioxidant activity was assessed through the DPPH and FRAP methods, and SPF value was determined with a UV/Vis spectrophotometer in the 290-390 nm wavelength range.

Results: The results showed that the retention time of quercetin was 16.648 min with a tailing factor of 1.623. The regression equation (y=224689x-989000) had a concentration range of 10-55 µg/ml and a correlation value of 0.9920. Limit of Detection (LOD) and Limit of Quantification (LOQ) were found to be 2.394±0.086 and 7.254±0.260 µg/ml, respectively. Method accuracy, determined by recovery values at concentrations of 50%, 100%, and 150%, ranged from 91.18% to 109.49%. Repeatability inter-day variations were expressed as %RSD values of 1.027-1.963% for AUC and 0.150-0.145 for RT. Moreover, the applied method showed stability within a temperature range of 14 °C–35 °C. Analysis showed gallic acid content of 1.773±0.049 mg/g in SNEDDS EAF formulation. Antioxidant activity measured through the DPPH and FRAP methods yielded IC₅₀ values of 4.167±0.552 µg/ml and 20.253±0.619 µg/ml, respectively, while SPF value at SNEDDS concentration of 150 µg/ml was 36.993±0.183.

Conclusion: This study successfully developed a precise, accurate, specific, and stable method for quantifying gallic acid levels in SNEDDS EAF of Melastoma malabathricum leaves in combination with Gentamicin. Therefore, SNEDDS EAF formulation exhibited an effective wound-healing potential, supported by a robust quality control process.

DESIGN, FABRICATION, IN VITRO, AND EX-VIVO PERMEATION STUDY OF MICRO-EMULSIFIED HYDROGEL OF FLUCONAZOLE (MHG-FLCZ) USING A CENTRAL COMPOSITE DESIGN (CCD)

2023-11-22T16:21:22+0530

Objective: The current study's objective was to develop and characterize a micro-hydrogel-based fluconazole (FLCZ) gel. A micro-hydrogel (Mhg) was prepared using different concentrations of Carbopol 940 (CP) and NaCMC using the modified swelling hydrogel method.

Methods: A Preformulation study was performed using FTIR to confirm the drug and polymers were compatible with each other based on the functional group determination. 3² optimization procedures were used to develop formulations based on the response surface methodology. The prepared formulations were evaluated for entrapment efficiency, spreadability, viscosity, and visual examination using binocular microscopy and in vitro drug release using Franz diffusion cells.

Results: The optimized formulation F2 reported entrapment efficiency of 65.09±0.41%, and viscosity of 11100±1.21 cps. The in vitro release of drug for the prepared formulations was performed for 8 h. and the optimized formulation showed better-controlled drug release compared to other formulations. It was observed that the optimized batch, percentage of drug permeability through the skin at 8 h of ex-vivo study shows 84.67±0.67% and in vitro drug release study (93.22%) through Franz diffusion cell, which suggests that the drug (Optimum batch) can easily penetrate through the skin and showed the highest drug release in a stipulated time interval.

Conclusion: The use of an optimized Mhg-FLCZ gel formulation as it has excellent homogeneity, a pH that is close to that of the skin, and suitable thixotropic characteristics relates to that much more convenience than the conventional dosage form. The in vitro and ex-vivo study data proved its suitability as a better alternative to conventional products in the effective treatment of skin infections.

FORMULATION AND CHARACTERISATION OF GASTRORETENTIVE IN SITU GEL LOADED WITH GLYCYRRHIZA GLABRA L. EXTRACT FOR GASTRIC ULCER

2023-08-06T17:54:33+0530

Objective: The study aimed to formulate and evaluate the gastroretentive in situ gelling system of Glycyrrhiza glabra L. extract to increase the gastric residence time and provide sustained release of the drug, thereby avoiding disadvantages such as frequent dosing, patient non-compliance and low bioavailability.

Methods: The in-situ gel was prepared by pH-triggered gelation method by using sodium alginate and gellan gum as polymers, sodium citrate as a crosslinking agent, and calcium carbonate as a floating agent. Formulation and optimization of in situ gels were achieved by 3² factorial design by using Design-Expert Software to determine the influence of independent variables such as concentration of sodium alginate and gellan gum on viscosity, gel strength, the onset of flotation, and drug release at 12 h.

Results: The viscosity, gel strength, onset of flotation and drug release at 12h of optimized formulation were found to be 568.89 cps, 42.91 sec, 53.17 sec and 82.69%, respectively. The floating duration of all in-situ gels was found to be more than 12 h. All the formulations showed drug content in the range of 83.55% to 95.28%. The in vitro release profile of the drug extract from all the formulations appeared to follow the Higuchi model, which concludes that the drug release was controlled by diffusion mechanism. The FTIR study indicates no chemical incompatibility between drug extract and other excipients.

Conclusion: Hence, a novel gastroretentive in situ gelling system of Glycyrrhiza glabra L. could be prepared for sustained oral delivery to increase patient compliance with reduced dosing frequency and increased residence time of the drug in the stomach.

LC-MS/MS-BASED QUANTITATIVE PROFILING OF PAPAIN ENZYME IN CARICA PAPAYA L.: METHOD DEVELOPMENT AND VALIDATION

2023-11-20T12:44:14+0530

Objective: To develop and validate a sensitive Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) method for quantifying the Papain enzyme in Carica papaya L. plant extracts.

Methods: As an internal standard (IS), Papain was procured. A gradient-based LC-MS/MS method was developed using the Quasar C₁₈, 150 mm × 2.1 mm, 3 µm column; the drug separation was accomplished using a gradient elution mode with a mobile phase consisting of 0.2% formic acid in water (A) and a 98:2% ratio of formic acid in acetonitrile (B). The mobile phase was injected with a volume of 10 µl at a flow rate of 0.5 ml/min.

Results: Matrix-matched calibration adhering to SANCO guidelines was employed for accurate quantification, covering a concentration range of 1 to 2000 ng/ml. The method's selectivity and linearity were confirmed with an R² correlation value of 0.990. Limits of detection (LOD) and quantification (LOQ) were determined as 170.5 ng/ml and 516.8 ng/ml, respectively. The developed LC-MS/MS method demonstrated robust analytical performance, providing a solid basis for quantifying Papain enzyme levels in Carica papaya L. plant extracts. The matrix-matched calibration approach, with a well-defined standard calibration curve, showcased the method's selectivity and linearity. The LOD and LOQ values further underscored the method's sensitivity.

Conclusion: This study successfully establishes and validates a gradient-based LC-MS/MS method for accurate quantification of Papain enzyme levels in Carica papaya L. plant extracts. The demonstrated precision, accuracy, and sensitivity support the reliability of this analytical approach, offering a valuable tool for future investigations into the biological effects of Papain.

APPROACH TO OPTIMIZE THE SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM FOR AZILSARTAN MEDOXOMIL USING BOX BEHNKEN DESIGN AND DESIRABILITY FUNCTION

2023-09-29T15:04:19+0530

Objective: Develop and optimize a novel self-micro emulsifying drug delivery system (SMEDDS) for enhancing the water solubility of Azilsartan (AZL) by employing the Box-Behnken design and the desirability function.

Methods: The formulation of AZL-SMEDDS consists of clove oil (oil component), Tween 20 (surfactant), propylene glycol (co-surfactant) as the independent variables and the active drug. Using a 3-level Design, the impact of independent variables on the formulation was examined. These variables' specified ranges are 20-40 mg, 50-80 mg, and 5-30 mg for X1, X2 and X3 respectively. Particle size (Y1), PDI (Y2), and dissolution % (Y3) were the response variables investigated in this study.

Results: The results indicated that the optimal values for Clove oil (X1), Tween 20 (X2), and Propylene glycol (X3) were determined to be 28.69, 76.45, and 24.93 (mg), respectively. Based on these optimized conditions, the predicted data points for the response variables Particle Size (Y1), Polydispersity (Y2), and dissolution % (Y3) were determined to be 59.85 nm, 0.729 and 55.406%, respectively.

Conclusion: The empirical results obtained from the optimized formulation exhibited a strong correlation with the predicted values. The optimized AZL-SMEDDS formulation demonstrated a rapid rate of drug solubility and greater bioavailability than AZL powder.

THE EFFECTIVENESS OF VARIOUS CITRONELLA OIL NANOGEL FORMULATIONS AS A REPELLENT OF AEDES AEGYPTI MOSQUITO

2023-12-05T04:49:18+0530

Objective: The aim of this research is to determine the effectiveness of the repellency of various citronella oil nanogel formulations against Aedes aegypti mosquito bites applied to guinea pigs.

Methods: The Citronella oil nanogel was prepared by emulsification technique combined with gelling formation. The nanoemulsion formula consists of 6% Citronella oil, 10% propylene glycol, 6% combination of Tween 80 and Span 80 in variation to 4 formula, and deionized water until 100%. Nanoemulsions were then added to the gel base which is composed of Carbopol 940 and TEA. The nanogel formed was characterized physically and its effectiveness against Aedes aegypti mosquito using guinea pigs as an animal model. The repellent activity was determined by the amount of mosquito bites on the guinea pigs’s skin.

Results: The organoleptic test displayed that all formulas comply with the requirements, except formula 1. The formula 2, 3, and 4 have particle size below 100 nm and the polydispersity index (PDI) less than 0.5. According to the repellent assay showed that all formulas have the effectiveness much higher than without the intervention. Formula 3 has the highest effectiveness of repellent activity against Aedes aedgypti in guinea pigs’ skin. The repellent activity of Formula 3 showed a significant difference (p-value of 0.005) as compared to nanogel without Citronella oil.

Conclusion: The protective power of Citronella oil nanogel Formula 3 is the most effective as compared to the other formula.

DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF LORATADINE SUSTAINED RELEASED BUCCAL FILM: IN VITRO AND IN VIVO STUDY IN BEAGLE DOGS

2023-12-15T15:05:04+0530

Objective: The aim of this work was to develop and evaluate bucco-adhesive films of Loratadine (LTD) for sustained release use.

Methods: Design of twelve different sustained released buccal film formulas using Carbopol, pectin, sodium alginate, glycerol, carboxymethyl cellulose (CMC), hydroxypropyl cellulose (HPC), Gelatin, Hydroxyethyl cellulose (HEC), and Hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers. Films were evaluated for physicochemical properties, thickness, swelling, moisture content, drug content, in vitro dissolution. The pharmacokinetic parameters of optimal formula were evaluated in beagle dogs.

Results: The selected film formula (F6) showed accepted content and muco-adhesion properties. The in vitro release study showed prolonged release of drug from films over 10 h in optimal formulation. The bioavailability studies performed using beagle dogs model showed that there was 113.45% increase in the AUC_0-24of selected film compared with oral market tablets.

Conclusion: Bucco-adhesive films is a promising dosage form for improving the bioavailability of loratadine.

DEVELOPMENT AND VALIDATION OF AN LC-MS/MS METHOD FOR THE DETERMINATION OF TENOFOVIR AND EMTRICITABINE

2023-10-23T17:31:31+0530

Objective: Therapeutic drug monitoring of tenofovir and emtricitabine, two commonly used antiretroviral drugs, is important to maximize effectiveness while minimizing side effects.

Materials: A Liquid Chromatography-Mass spectrometry (LC-MS/MS) method was developed to quantify tenofovir and emtricitabine in human plasma samples. The method involves a simple solid phase extraction procedure followed by liquid chromatography separation using a Penta Fluoro Phenyl (PFP) column with a Phenomenex C18 column and a mobile phase of ammonium formate, acetonitrile, and methanol, achieving separation in under 4 min.

Results: The method showed good accuracy, low limits of quantification, adequate recovery, minimal matrix effects, and specificity. Analyte stability under multiple storage conditions was demonstrated.

Conclusion: The validated LC-MS/MS method provides a reliable tool for therapeutic drug monitoring and pharmacokinetic studies of anti-Human Immuno-deficiency Virus (HIV) regimens. The assay can be applied to large populations, especially in resource-poor settings, to help individualize dosing and improve clinical outcomes while reducing toxicity.

STATISTICAL OPTIMIZATION AND EVALUATION OF IN SITU GEL FOR THE OCULAR DELIVERY OF CROMOLYN SODIUM

2023-11-02T14:33:42+0530

Objective: The study aimed to develop and optimize cromolyn sodium-based ocular in situ gel to improve the ophthalmic contact period and provide sustained drug release for treating allergic conjunctivitis.

Methods: Formulations were prepared using sodium alginate and HPMC K4M (Hydroxypropyl Methylcellulose) polymers and were characterized and evaluated for viscosity, gelling time, in vitro drug release, and optimized using a factorial 3²DOE design (Version 11; Design Expert^® software). The resulting cromolyn sodium-based formulation was tested for hyperemia and eye-scratching behavior in Wistar albino rats.

Results: Increased polymer concentrations resulted in higher viscosity with decreased gelling time and in vitro drug release. The optimized formulation achieved a viscosity of 15.350 cps, a gelling time of 55.137 s, and sustained drug release of 92.61% over 12 h. The in vivo pharmacodynamic study of the optimized formulation showed a significant decrease in the frequency of eye-scratching behaviour (7.525) at a significance level of (**p<0.01) and hyperemia (1.125) (***p<0.001, *p<0.05) compared to negative and positive control indicating that the developed in situ formulation improved the drug's therapeutic effectiveness by extending its duration within the cul de sac.

Conclusion: In light of these findings, this optimized cromolyn sodium in situ gel holds promise as a viable alternative to conventional eye drops

CHARACTERISATION, EVALUATION AND DENSITY FUNCTIONAL ANALYSIS OF CILNIDIPINE-NICOTINAMIDE COCRYSTALS DEVELOPED BY LIQUID ASSISTED GRINDING TECHNIQUE: A SUSTAINABLE APPROACH FOR ENHANCED SOLUBILITY

2023-11-13T01:31:06+0530

Objective: Improving the solubility of poorly water-soluble drugs has always been a challenge in drug development. This study aimed to enhance the aqueous solubility of a poorly water-soluble drug, Cilnidipine, by cocrystallisation method using liquid-assisted grinding (LAG) technique with Nicotinamide as the coformer. The study also aimed to understand the mechanism of cocrystal formation by quantum mechanical calculations.

Methods: The Cilnidipine-Nicotinamide cocrystals were prepared in various stoichiometric ratios using the liquid-assisted grinding (LAG) technique. The cocrystals obtained were characterised by vibrational spectroscopy, thermal methods such as differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and surface morphology by field emission scanning electron microscopy (FE-SEM). The cocrystals were evaluated for saturation solubility, and the mechanistic study of cocrystal formation was performed using the Gaussian 09 software package.

Results: FT-IR spectra of the formulated cocrystal indicated the intermolecular hydrogen bond formation between-N-H of Nicotinamide and the nitro group of Cilnidipine. DSC analysis showed a single endotherm at 96.76 °C, PXRD patterns were different from that of the reactants, and FE-SEM analysis revealed the changes in the surface morphology of the obtained cocrystal. The prepared cocrystal showed a 26.36-fold enhancement in the aqueous solubility of Cilnidipine. The DFT study demonstrated the formation of a strong intermolecular hydrogen bonding between the nitro-oxygen atom of Cilnidipine and the amide hydrogen atom of Nicotinamide in cocrystal formed.

Conclusion: This study highlights the potential of the liquid-assisted grinding method for preparing cocrystals as a sustainable and reliable approach to address the challenges posed by poorly water-soluble drugs.

SOLUBILITY ENHANCEMENT OF ATAZANAVIR BY HYDROTROPIC SOLUBILIZATION TECHNIQUE

2023-11-18T13:35:13+0530

Objective: The present study aims to increase the solubility and dissolution of atazanavir sulfate (ATZ) by employing a hydrotropic solubilization technique.

Methods: ATZ is a poorly soluble drug classified under the biopharmaceutical classification system (BCS)-II, which accounts for its poor oral bioavailability. Different hydrotropic agents, such as urea and sodium benzoate and their combinations at different ratios were prepared. The prepared hydrotropes were systematically investigated for compatibility between the drug and excipients using Fourier Transform Infra-Red Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) approaches. Further, in order to understand the conversion from crystalline to amorphous nature, X-ray Diffraction (XRD) and Scanning Electron Microscopy (SEM) studies were also performed. The formulation of a mixed hydrotropic mixture comprising urea (2.5% w/v) and sodium benzoate (5% w/v) exhibited a 100.35±1.7 % drug release at 0.25 h with higher dissolution efficiency as compared with other batches of individual hydrotrope, mixed hydrotropes as well as pure drug.

Results: FTIR studies revealed that there is no incompatibility between the drug and the selected hydrotropes. DSC studies also confirmed the fact that there is no interaction between the drug and the hydrotropes by the disappearance of an endothermic peak. XRD studies revealed that there was a significant reduction in the intensity of peaks, indicating the conversion of crystalline to the amorphous form. The SEM studies indicated that the drug appears crystalline in the shape of an irregular tiny prismatic needle, indicating its crystallinity. At the same time, the hydrotrope mixtures appeared in agglomerated form with a porous nature, which may be accountable for its increase in solubility. The hydrotropes prepared using urea alone exhibited an increase in solubility of 4.42 folds, and the hydrotrope prepared using sodium benzoate alone exhibited an increase in solubility of 3.178 folds; the combination hydrotropes of urea and sodium benzoate exhibited an increase in solubility of 8.78 folds in water as compared to pure drug. The drug release from the mixed hydrotropes obeys zero-order kinetics with diffusion as the main mechanism.

Conclusion: The present investigation concluded that the combination of hydrotropes enhanced the solubility of the aqueous soluble drug ATZ. However, in vivo studies are essential to establish its potential effect.

DEVELOPMENT AND EVALUATION OF NANOBIOCOMPOSITE TOPICAL FORMULATION

2023-10-05T19:01:04+0530

Objective: The proposed research involving transferosomes within a hydrogel matrix offers a promising approach for enhanced wound healing. This system aims to facilitate the dermal delivery of nanosized curcumin while incorporating Ascorbic acid and Salicylic acid. The integration of these components holds the potential for advancing chronic wound therapy.

Methods: Curcumin transferosomes were formulated by the lipid thin film hydration method and further optimization was carried out using 3² full factorial design. The transferosome formulation, prepared using phospholipon 90G, involved selecting specific variables: the quantity of edge activator and sonication duration as independent factors, while the optimization process considered particle size and entrapment efficiency as dependent variables. Following the optimization of the transferosomes, a hydrogel formulation was developed using the central composite design approach.

Results: Optimized transferosome (Batch F8) showed 87.75±3.74 nm (nanometer) particle size and 91.18±2.71% entrapment efficiency. Hydrogel was formulated by Central composite design, selecting pH and spreadability as dependent factors, to which was added curcumin transferosomes, Ascorbic acid and Salicylic acid. The data was analyzed using Stat-ease Design-Expert v7.0.0 software. The optimized batch F3 showed a pH of 6.84, spreadability of 12.89 gm. cm/sec and Curcumin release of 87.47%. Drug release from nanobiocomposite hydrogel was evaluated using the in vitro study of the formulation. The various kinetic models were applied to in vitro release data for the prediction of the drug release kinetic mechanism. The release constants were calculated from the slope of appropriate plots, and the regression coefficient (R²) was determined. It was found that the in vitro drug release of the formulation was best explained by Higuchi as the plots show the highest linearity. The regression coefficient (R²) was found to be 0.907, 0.9266 and 0.9536 for Ascorbic acid, Salicylic acid and Curcumin, respectively.

Conclusion: The nanobiocomposite topical formulation was thus prepared, tested and for skin irritancy study. There is no noticeable signs of erythema, edema, or inflammation were observed on the skin. These results indicate that the developed transdermal formulation does not cause skin irritation and can be considered non-irritating.

APPROACHES ON SURROGATE METHODS FOR IN VIVO BIOEQUIVALENCE STUDY OF FORMULATED BILAYER TABLETS OF DOMPERIDONE AND ITOPRIDE

2023-10-17T12:27:49+0530

Objective: This study aims to provide a more efficient pathway for generic drug approval while maintaining the same level of therapeutic equivalence and safety as the reference product. This was based on the equivalence of in vitro evidence other than through expensive in vivo equivalence testing.

Methods: Biowaiver and IVIVC are surrogate methods for in vivo bioequivalence studies. The Biowaiver test was done according to WHO, TRS992, 2015 Annex 7, Appendix 1, the recommendation for conducting and assessing comparative dissolution. IVIVC was done by the level A Convolution method. Innovator product was used as Ganaton OD for Itopride and Motilium for Domperidone to perform the comparison testing.

Results: The similarity factor (F2) between the test and innovator product of Domperidone at pH 1.2 HCl, Acetate Buffer pH 4.5, and water was 79.51, 68.00, and 58.97 and the dissimilarity factor (F1) was 7.24, 8.05 and 11.01 respectively. From the IVIVC study by level A convolution method of C_max, AUC, T_max of Ganaton OD and formulated Itopride were found to be 409.16ng/ml, 5652.28 ngh/ml and 4h and 252.16ng/ml, 4601.12 ngh/ml and 12 h respectively.

Conclusion: The F2 limit is 50-100 and F1 is 15 mentioned as per guidelines followed for the biowaiver test, which means the formulated domperidone is deemed equivalent to (Motilium) innovator of domperidone. The predictive error on the AUC of Itopride formulated was found to be 18.59 % which was within the limit of±20 %, demonstrating the therapeutic range.

EXPLORATION OF ANTI-MELANOMA POTENTIAL OF PHYTOCHEMICALS FROM NYCTANTHES ARBORTRISTIS THROUGH COMPUTATIONAL STUDIES

2023-11-08T14:19:34+0530

Objective: The goal of the current research is to identify the dominant phytochemical from the plantNyctanthesarbor-tristis Linn. and to investigate their binding affinities against the proteins BRaf Kinase mutant (3OG7) and Hsp90 Chaperone (2VCJ) that causesmelanoma.

Methods: In this work, Schrodinger software was utilized to investigate the anti-cancer potential of phytochemicals Nyctanthesarbor-tristis against specific target proteins, namely BRaf Kinase mutant (3OG7) and Hsp90 Chaperone (2VCJ) Inhibitors.

Results: Based on the outcome of the docking investigation, phytochemicals that exhibited highest binding affinity to the specified protein targets were subjected to induced fit docking and MM-GBSA computations using the Schrodinger Maestro version 2021.2 in prime module. According to the analysis, the compounds with the highest binding affinities for 2VCJ and 3OG7 are Arbortristoside D and Nicotiflorin respectively. The compound that interacted with both the proteins wasArbortristoside B. These phytochemicals appear to be more effective to the FDA-approved V600E-BRaf inhibitor Vemurafenib and Hsp90 Chaperone Inhibitor Diclonine.

Conclusion: One of the most common, deadly, and dangerous malignant diseases with a high global prevalence rate is melanoma (skin cancer). The present study may prove more helpful in developing an ideal targeted drug delivery system of phytochemicals obtained from plant Nyctanthesarbor-tristisfor treatment of melanoma. This suggests that these substances could be evolved into highly effective anti-melanoma drugs.

DEVELOPMENT OF A REFERENCE SAMPLE FOR RAPID ANALYSIS OF AN ELEMENTAL COMPOSITION OF MEDICINAL PLANT RAW MATERIALS

2023-11-22T17:29:00+0530

Objective: Development and validation of a technique for preparation of a reference sample for elemental microanalysis using the XRF technique in terms of repeatability, reproducibility, and optimization of the technique for rapid determination of the elemental composition of medicinal plants based on X-ray fluorescence analysis.

Methods: Samples: fresh shoots of Kalanchoe daigremontiana, ready reference sample "Birch Leaf" LB-1 (A. P. Vinogradov Institute of Geochemistry, Siberian Branch of the Russian Academy of Sciences, Irkutsk, Russia), and IAEA reference sample SRM 2976 (IAEA, MEL, Monaco). The dispersed fraction was analyzed using a Master Sizer 2000 instrument (Malvern Panalytical, Worcestershire, UK). Elemental analysis using an energy dispersive X-ray fluorescence spectrometer EDX-7000 Shimadzu (Shimadzu Corporation, Kyoto, Japan), GZ-AAS using an Agilent instrument, model 240Z AA instrument (Agilent Technologies, Inc., Santa Clara, USA) with electrothermal atomization and Zeeman background correction, and ICP-MS using an Agilent 7500 CE instrument (Agilent Technologies, Inc., Santa Clara, USA).

Results: By the LALLS method, they were separated by the maximum distribution, which was 63 microns, and a minor fraction of 39 microns. This indicates sufficient homogeneity in the sample. Further, homogeneity was proved by the XRF method by measuring six independent samples obtained by the quartering method. Also, the elemental composition of the reference samples was determined: completely dried, homogenized before sifting, and homogenized after sifting. Further, the obtained reference sample of K. daigremontiana was compared with reference samples: IAEA SRM 2976 and "birch leaf methods: ICP-MS, GZ-AAS, XRF.

Conclusion: The reference sample will allow for rapid analysis of medicinal plant raw materials. Standardization of medicinal plants by the content of microelements will allow observing species differences as well as adjusting the concentrations of microelements for therapeutic purposes using medicinal plants.

AZITHROMYCIN AND OSELTAMIVIR QUANTIFICATION METHOD DEVELOPED AND VALIDATED USING LIQUID CHROMATOGRAPHY-TANDEM MASS SPECTROMETRY IN DRIED BLOOD SPOT

2023-08-04T08:39:48+0530

Objective: The development and use of bio-sampling techniques for the analysis of COVID-19 drugs oseltamivir and azithromycin using the Dried Blood Spot technique simultaneously using LC-MS/MS aims to obtain optimal conditions and validated analytical methods using LC-MS/MS according to Food and Drug Administration 2018 recommendations.

Methods: Azithromycin and oseltamivir analyses were performed using LC-MS/MS with C18 Acquity® Bridged Ethylene Hybrid (BEH) column 1.7 m, 100 x 2.1 mm. The matrix sample used is Dried Blood Spot (DBS) with azithromycin and Oseltamivir as the raw material and acyclovir as the internal standard. Optimum analytical conditions were obtained on a gradient mobile phase using 0.1% formic acid-methanol solution with a flow rate of 0.2 ml/minute. The quantification of the analysis was carried out using triple quadrupole mass spectrometry with positive electrospray ionization (ESI) mode.

Results: The calibration curve ranged from 0.5 to 160 g/ml, and the Lower Limit of Quantification (LLOQ) achieved was 25.31 and 25.37 ng/ml. Sensitivity, selectivity, linearity, precision, carry-over, accuracy, stability, and recovery were found to be within the suitable limits and fully validated by the guidelines from the Food and Drug Administration 2018.

Conclusion: The method developed successfully passed all of the FDA's 2018 full validation guidelines, with the LLOQ achieved for azithromycin and Oseltamivir was 25.31 and 25.37 ng/ml.

IN SILICO EXPLORATION OF BERBERINE AS A POTENTIAL WOUND HEALING AGENT VIA NETWORK PHARMACOLOGY, MOLECULAR DOCKING, AND MOLECULAR DYNAMICS SIMULATION

2023-11-23T17:16:20+0530

Objective: Wound healing remains a complex biological process crucial for tissue repair and homeostasis. Our goal in this paper is to focus on the application of advanced computational techniques to explore the potential of naturally occurring compound berberine in addressing molecular targets related to wound healing.

Methods: Network pharmacology, molecular docking analysis, in silico ADMET prediction, and extensive 100 ns molecular dynamics simulations was performed to gain a holistic understanding of the therapeutic potential of berberine against molecular targets involved in wound healing. This study predicted drug-likeness scores, potential side effects, ADMET profiles, carcinogenicity, MolLogP, molecular volume analysis, and molecular polar surface area for berberine.

Results: Findings of the study revealed that berberine displayed a remarkable binding affinity for the epidermal growth factor receptor (EGFR), with a binding energy of-8.14 kcal/mol, surpassing the crystal ligand's binding energy of-7.15 kcal/mol. This indicates a strong potential for berberine in modulating EGFR-related pathways critical for wound healing. The culmination of the investigation was a 100 ns molecular dynamics simulation, which demonstrated consistent binding and stability over time, reinforcing the potential of berberine as a wound healing agent.

Conclusion: The integration of gene expression analysis, enrichment studies, network analysis, molecular docking, and molecular dynamics simulations unveiled crucial mechanisms underlying efficacy of berberine as a potent wound-healing agent.

FORMULATION AND EVALUATION OF SUSTAINED-RELEASE FLOATING MATRIX TABLETS OF VALGANCICLOVIR HYDROCHLORIDE

2023-09-29T17:14:59+0530

Objective: The present study aimed to formulate and evaluate the formulated sustained-release floating matrix tablets of valganciclovir hydrochloride to produce a stable and bioavailable dosage form.

Methods: The tablets were prepared using hydrophilic and hydrophobic polymers such as ethyl cellulose, Hydroxy-propyl methylcellulose (HPMC), and Povidone. The formulations were subjected to evaluation characteristics such as drug content, hardness, friability, floating lag time, total floating time, and In vitro drug dissolution studies.

Results: The formulation composition and method of manufacturing are novel for this particular active moiety and robustness was assessed using a central composite design. All the formulation trials exhibited more than 90% of drug release in 12 h duration, with a floating lag time of more than 11 h, and drug content was found more than 90% across the batches. The hardness and friability profiles were found to be uniform across the batches. The preliminary evaluation confirms the received drug is pure and FTIR results show that the drug and excipients are compatible. The hardness and friability profiles were found consistent across the batches. All the formulation trials of central composite design have shown more than 90% of drug release in 12 h duration, with a floating lag time of more than 11 h, and drug content was found more than 90% across the batches.

Conclusion: The formulated valganciclovir hydrochloride sustained release floating matrix tablets showed an increased GRT with a sustained release for 12 h, thereby allowing a better window for absorption and consequently improving the drug's therapeutic effect.

STUDY ON FORMULATION OF BACTERIAL CELLULOSE NANOFIBERS-COATED NANOLIPOSOMES CONTAINING PACLITAXEL FOR ORAL ADMINISTRATION

2023-12-06T01:01:44+0530

Objective: The low oral bioavailability of paclitaxel (PAC) because of its limited aqueous solubility and poor intestinal permeability after being administered orally suggests the need for a sustained release system. The aim of this study is to produce and evaluate in vitro a nanoliposome system that carries paclitaxel (BCN-LIP-PAC) for oral administration.

Methods: Thin-film evaporation and electrostatic deposition methods were used to obtain LIP-PAC and BCN-LIP-PAC. Particle size, polydispersity index (PDI), zeta potential, morphological analysis, entrapment efficiency percentage (EE%), and in vitro dissolution studies were used to characterize the developed systems.

Results: The nano-range sizes of LIP-PAC and BCN-LIP-PAC (0.1 % BCN) were 112±4.2 nm and 154±6.4 nm, respectively, where EE % were 80.6±2.3 % and 84.6±1.7 %, respectively. BCN-LIP-PAC exhibited good stability in simulated gastrointestinal ﬂuids. The drug release experiments conducted in vitro showed that BCN-LIP-PAC had obvious sustained release behaviors when compared to LIP-PAC. Furthermore, the release rate of PAC from all LIP-PAC and BCN-LIP-PAC was higher in SIF than in SGF.

Conclusion: The preparation, characterization, and evaluation of BCN-LIP-PAC (0.1 % BCN) for oral PAC delivery were all successful. In conclusion, the approach presented herein is a promising option for delivering oral sustained-release PAC.

FORMULATION, ANALYSIS AND VALIDATION OF NANOSUSPENSIONS-LOADED VORICONAZOLE TO ENHANCE SOLUBILITY

2023-10-19T12:57:10+0530

Objective: This study aimed to enhance the solubility of voriconazole (VRZ) via loading to nanosuspensions using solvent/anti-solvent technique. The optimisation of independent variables (polymer concentrations) was carried out to achieve the desired particle size and maximise the percentage of entrapment efficiency (EE %) and drug loading (DL %) using design-expert^®software.

Methods: Design-Expert^® software, version 13, was used to design and optimise nanosuspensions-loaded VRZ using 2³ factorial designs. Concentrations of polyvinylpyrrolidone, hydroxypropyl methylcellulose and poloxamers were selected as independent variables to achieve ideal particle size, polydispersity index (PDI), entrapment efficacy (EE %) and drug loading (DL %). Atomic force microscopy (AFM), differential scanning calorimetry (DSC) and saturated solubility were used to assess the lyophilized nanoparticles. The compatibility between the drug and the polymers was studied using Fourier transform infrared spectroscopy (FTIR).

Results: The particle size, PDI, EE %, and DL % were in the range of 15.6–145.6 nm, 0.010-0.120, 55.9 %-91.9 %, and 6.68-36.76 %, respectively. The saturated solubility of nanosuspensions-loaded VRZ (NS-VRZ) relative to free VRZ was increased tenfold in DW and twelvefold in PBS (pH 7.4). DSC thermogram confirmed the incorporation of VRZ in the nanosuspensions. The AFM of NS-VRZ validated spherical tiny particle size with a smooth surface. There is no chemical interaction between VRZ and the polymers, according to an FTIR investigation.

Conclusion: The solubility of VRZ was successfully enhanced by loading to nanosuspensions. The solvent/anti-solvent technique was proven to be cost-effective, easy to operate and suitable for the preparation of NS-VRZ using Design-Expert^®software.

DECODING THE THERAPEUTIC POTENTIAL OF EMPON-EMPON: A BIOINFORMATICS EXPEDITION UNRAVELING MECHANISMS AGAINST COVID-19 AND ATHEROSCLEROSIS

2023-12-18T10:00:40+0530

Objective: This study aims to elucidate the main compounds and mechanisms of action of Empon-empon (EE), a traditional Indonesian herb used for treating COVID-19 and atherosclerosis, utilizing an integrated network pharmacology and molecular docking approach.

Methods: Active compounds in EE were obtained through the KNApSAcK, screening active compounds using parameters: oral bioavailability (OB) ≥ 30% and drug-likeness (DL) ≥ 0.18. Compound-related target genes were collected from GeneCard, ChemBL, and Traditional Chinese Medicine Systems Pharmacology (TCMSP). Disease targets were obtained from the GeneCard database. The protein-protein interaction (PPI) network was built using STRING and visualized using Cytoscape. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis using ShinyGO. Molecular docking analysis using Autodock Vina in PyRx.

Results: We identified 18 main compounds in EE. PPI analysis obtained 5 central EE targets involved in treating COVID-19 and atherosclerosis, namely E1A Binding Protein P300 (EP300), Heat Shock Protein 90 Alpha Family Class A Member 1 (HSP90AA1), SRC Proto-Oncogene (SRC), Estrogen Receptor 1 (ESR1), and RELA Proto-Oncogene (RELA). GO and KEGG analysis illustrated EE's pharmacological effects through pathways in cancer, lipid and atherosclerosis, and PI3K-Akt signaling, including Coronavirus disease. Catechin and quercetin exhibited the strongest binding affinity to EP300; licarin B and delphinidin to HSP90AA1; epicatechin and delphinidin to SRC; galangin and ellagic acid to ESR1; and guaiacin and licarin B to RELA.

Conclusion: This research provides a strong foundation regarding the main compound and mechanism action of EE in treating atherosclerosis and COVID-19, suggesting potential as a novel therapeutic agent.

PREPARATION AND JUSTIFICATION OF NANOFIBRES-LOADED MAFENIDE USING ELECTROSPINNING TECHNIQUE TO CONTROL RELEASE

2023-10-24T22:47:09+0530

Objective: The primary objective was to fabricate a novel drug delivery system capable of providing a controlled and prolonged release of antibiotics.

Methods: The experimental design was formulated using Design-Expert® software (version 13), enabling systematic and efficient fabrication process optimization. The study involved the preparation of various nanofiber formulations with different ratios of the three polymers to assess their impact on drug release behavior. Mafenide, a widely used antibiotic, was chosen as the model drug for this investigation. The electrospinning process allowed for producing uniform and fine nanofibers with a high surface area, ensuring a large drug-loading capacity. The synthesized nanofibers were characterized using scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) to evaluate their morphology, chemical interactions, and thermal properties. The drug release kinetics of the antibiotic-loaded nanofibers were studied under different physiological conditions to assess their sustained release behavior.

Results: The final nanofiber formula was successfully prepared using the electrospinning technique. The Fourier Transform Infrared Spectroscopy (FTIR) analysis was achieved to confirm the possibility of chemical interaction and bond formation between mafenide and the polymers. Present. The SEM picture of the optimized nanofiber formula showed the homogeneity and excellent entanglement of the electrospun nanofibers at a resolution of 5 µm. PVA/chitosan/HPMC and mafenide pure drug have been successfully fabricated with sufficient strength to resist swelling after absorbing wound exudate. The polymer network becomes more compact when chitosan and Hydroxypropyl Methyl Cellulose (HPMC) are combined with polyvinyl alcohol (PVA), enabling regulated swelling during solvent ingress. The polymer composite's three-dimensional network influenced how quickly the medication was released from the matrix. Sample 2's polymer network traps the medication, gradually releasing after controlled swelling, resulting in a sustained release profile compared to blank sample according to the cumulative release (%) study of mafenide loaded nanofiber and mafenide drug blank sample.

Conclusion: This research successfully demonstrated the fabrication of sustained-release antibiotic nanofibers using electrospinning and three biocompatible polymers. The systematic optimization approach using Design-Expert® software proved effective in tailoring the drug release behavior of nanofibers. The developed drug delivery system holds great promise for pharmaceutical applications, particularly in improving antibiotic therapies and patient care.

EPLERENONE FLOATING MICROSPHERES: RADIOGRAPHIC AND PHARMACOKINETIC STUDIES IN RABBITS

2023-11-04T11:52:51+0530

Objective: The objective of the present investigation was to evaluate gastro-retentive performance and pharmacokinetic parameters of Eplerenone-optimized floating microspheres compared with formulated floating tablets.

Methods: Microsphere contains antihypertensive drug Eplerenone as a core material encapsulated with the polymeric membrane for sustained drug release were prepared by solvent diffusion-evaporation technique. The prepared microspheres were evaluated for qualitative and quantitative parameters. The optimized formulation showed favorable in vitro floating and drug release profile. The gamma scintigraphy of the formulation was carried out in rabbit in order to determine the floating ability of the final formulation with barium sulfate. Prolonged gastric residence time of over 12 h was achieved in all the animals. Eplerenone-loaded optimized formulation was orally administered to rabbit and blood samples were used to determine pharmacokinetic parameter by using WinNonlin software 3.0 version.

Results: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the Floating tablet showed improved parameters of Cmax; similarly, time to reach peak plasma concentration (t-max) for Eplerenone Floating microspheres was 4 times increased against Floating tablet formulation. The area under the curve (AUC) for formulated floating tablet was found to be 9.69 µg/ml, whereas for floating microspheres it was 16.28 µg/ml, for formulated floated tablet absorption rate constant Ka was 1.61 h, elimination rate constant was 0.112 h and elimination half-life 6.2 h. The comparison of these data undoubtedly shows that the Cmax was not much valid, but AUC was increased to about 1.68 times in case of floating microspheres, absorption rate constant was found to be decrease 3.22 times when related to the floating microspheres, whereas Ke was found to be decrease 2.11 times when equated to floating microspheres, elimination half-life was increased by almost about two times.

Conclusion: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the floating tablets showed enhanced parameters of the formulated due to floating nature of the present designed formulation.

EXPLORATION OF THE ACTIVE COMPOUNDS OF MORINGA OLEIFERA LAM AS HIV-1 REVERSE TRANSCRIPTASE INHIBITOR: A NETWORK PHARMACOLOGY AND MOLECULAR DOCKING APPROACH

2023-11-13T22:19:46+0530

Objective: This study aims to predict the active compound of Moringa oleifera for the treatment of Human Immunodeficiency Virus (HIV), specifically targeting the HIV-1 reverse transcriptase (HIV-1 RT) enzyme using network pharmacology and molecular docking approach.

Methods: The active ingredients of M. oleifera, were screened from the Knapsack database. Subsequently, HIV-1 RT and its related target compounds were retrieved from the Genecard database. The analysis of common targets involved protein-protein interactions (PPI) analysis using string databases and constructing interaction IDs using Cytoscape software. Gene Ontology (GO) functional and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed. Molecular docking studies were conducted using AutoDock Vina software to validate the results of the network pharmacological analysis.

Results: A total of 63 active ingredients and 8601 targets related to HIV-1 RT were identified. The network analysis, encompassing GO and KEGG enrichment, revealed strong associations of common targets with key signaling pathways such as Tumor Necrosis Factor (TNF), Toll Like Receptor (TLR), and apoptosis. Additionally, 11 compounds of M. oleifera including apigenin, benzyl isothiocyanate, benzylamine, caffeic acid, ferulic acid, epicatechin, kaempferol, gallic acid, luteolin, syringic acid and vanillin were identified as potential vital compounds. Molecular docking analysis highlighted apigenin and kaempferol as the most promising compounds, exhibiting the lowest binding affinity to the HIV-1 RT enzyme. These compounds correlated with caspase-3(CASP3), caspase-9 (CASP9), and BCL2 Apoptosis Regulator (BAX) protein, stimulating cell apoptosis through multiple pathways.

Conclusion: The study highlighted that apigenin and kaempferol are potential compound of M. oleifera in HIV-1 treatment through inhibition activity at HIV-1 RT Enzyme.

ANTIVIRAL ACTIVITY OF SAUSSUREA LAPPA ETHANOL EXTRACT AGAINST SARS-COV-2: IN VITRO STUDY

2023-11-19T21:36:12+0530

Objective: The study aims to investigate the antiviral activity of S. lappa against Severe Acute Respiratory Syndrome-Coronavirus 2 (SARS-CoV-2) in vitro.

Methods: The extracts are obtained by ultrasonic-assisted extraction (UAE) with a 96% ethanol solvent. Thin-layer chromatography (TLC) uses n-hexane: ethyl acetate and chloroform: methanol) as mobile phases. The staining outcome is subsequently examined using UV visualizers with a wavelength of 366 nm. To assess the antiviral activity of Vero E6 cells, extracts were employed at doses of 25, 50, 75, and 100 µg/ml, with remdesivir serving as the positive control. Supernatants were collected on days 1, 2, 3, and 6 for qRT-PCR testing with target genes E and ORF1ab. Time-addition experiments were conducted to determine how the extract works as antiviral. Protein expression was tested with Western blots with antibodies S and N SARS-CoV-2.

Results: TLC identifies terpenoid chemicals present in the ethanol extract of S. lappa. The ethanol extract of S. lappa exhibited antiviral effects against SARS-CoV-2, with an inhibitory concentration 50 (IC₅₀) of 40 µg/ml, a cytotoxic concentration 50 (CC₅₀) of 131.4 µg/ml, and a selectivity index of 3.51. The extract can potentially impact the entry-post-entry phase of SARS-CoV-2 infection in Vero cells. The immunoblotting results demonstrated a reduction in the expression of S and N proteins in the treatment group compared to the negative control.

Conclusion: S. lappa ethanol extract has antiviral activity against SARS-CoV-2 based on an in vitro study.

MODIFYING FRACTION EXTRACTED FROM SESEWANUA (CLERODENDRUM FRAGRANS WILD) LEAVES IN SNEDDS PREPARATIONS: CHARACTERIZATION AND BIOAVAILABILITY TEST

2023-09-14T04:45:45+0530

Objective: This study aimed to determine the effect of compound modification using acyl chloride derivatives on n-hexane: ethyl acetate fraction of sesewanua leaves, focusing on the characteristics and pharmacokinetics profile in Self-Nano-emulsifying Drug Delivery System (SNEDDS) preparations.

Methods: A quasi-experimental method was used with six SNEDDS formulas, namely F0 (without active substance), F1 (acetyl chloride fraction), F2 (propanoyl chloride fraction), F3 (butyryl chloride fraction), and F4 (pentanoyl chloride fraction) and F5 (piperine compound). The fractions were subjected to characterization tests, including particle size, polydispersity index, and zeta potential as well as determination of pharmacokinetics profile using the modified crane and Wilson method.

Results: The results showed that the characterization tests of particle size using Particle Size Analyzer (PSA) for F0-F5 on gastric fluid included 15.8, 17,367, 20,367, 15.8, 28.233, and 21.533 nm. The polydispersity index values were 0.211, 0.438, 0.311, 0.383, 0.394, and 0.397, while the Zeta Potential values were-22,267,-22.2,-23.5,-24,033,-22,967, and-21.6 mV, respectively. The pharmacokinetics profile of AUC0-∞ was as follows: F0 0 μg, F1 492.83, F2 492.83, F3 245.98, F4 492.94, and F5 843.38 μg. Fraction five (F5) as a control had a higher AUC0-∞ value than compared to the fractions modified with acyl chloride derivatives. The T1/2 elimination values were F0 0 h, F1 22.5 h, F2 10.811 h, F3 35.54 h, F4 231.01 h, and F5 15.469 h.

Conclusion: Based on the results, the addition of acetyl, propanoyl, butyryl, and penthanoyl chloride affected Particle Size Characterization Analysis and pharmacokinetics profile of SNEDDS preparation of n-hexane: ethyl acetate fraction. Structural modification showed the ability to alter the bioavailability of the active ingredient according to the desired therapeutic goal.

NANOENCAPSULATION OF ETHANOL EXTRACT OF PAPAYA LEAF (CARICA PAPAYA LINN.) USING CHITOSAN AND TESTING ITS EFFECTIVENESS AS AN ANTI-INFLAMMATORY

2023-11-28T03:56:57+0530

Objective: Papaya is a plant typical of West Kalimantan which has many properties such as anti-inflammatory, analgesic, antimalarial, and antibacterial. This research aims to formulate ethanol extract of papaya leaves into a nanoencapsulated preparation and test its effectiveness as an anti-inflammatory.

Methods: Nanoparticle formulations made with the ionic gelation method use polymer chitosan (0.25%-1%) with crosslinker sodium tripolyphosphate (0.25%). Nanoencapsulation ethanol extract of papaya leaf was evaluated for characteristics including particle size distribution, index polydispersity, zeta potential, particle morphology, and entrapment efficiency. Furthermore, The efficacy of anti-inflammatory nanoencapsulation was then evaluated on male Wistar rats with carrageenan-induced inflammation using doses of 100 mg/kg and 200 mg/kg. The assessment of anti-inflammatory activity utilized the Rat hind paw edema method by observing the development of inflammation in the volume of the soles of the test animals' paws.

Results: The results of nanoencapsulation characterization showed that papaya ethanol extract in Formula 1 with a ratio of Chitosan: Papaya Leaf Extract Ethanol: NaTPP = 6:1:1 was the best formula, exhibiting an average particle size of 217.3±47.8 nm, a polydispersity index value of 0.271, a zeta potential value of+34.3 mV, an entrapment efficiency value of 65.54, and a particle morphology that is less spherical. The test for anti-inflammatory activity of papaya leaf ethanol extract nanoparticles, administered orally at a dosage of 200 mg/kgBW, demonstrated the highest percentage of anti-inflammatory efficacy at 61.538%. In comparison, the positive control group (diclofenac sodium) exhibited 54.325%, and the low-dose group (100 mg/kgBW) showed 51.585%. The results showed that the ethanol extract of papaya, when nanoencapsulated in chitosan nanoparticles, exhibits good characteristics and has significant potential for inhibiting inflammation in male Wistar rats induced by carrageenan.

Conclusion: The characterization results of the optimal chitosan-ethanol papaya leaf extract nanoparticles were obtained using Formula 1. Nanoparticles of chitosan-ethanol extract from papaya leaves at doses I and II exhibited anti-inflammatory activity that was not significantly different.

DESIGN AND IN VIVO EVALUATION OF NAPROXEN-LOADED TRANSFEROSOMAL GEL FOR TRANSDERMAL DELIVERY

2023-10-06T08:41:35+0530

Objective: The main objective of the present study was to formulate, optimize, and evaluate naproxen transfersomal gels.

Methods: Reverse phase evaporation was used to create thirteen different formulations of naproxen-loaded transfersomes. Using Response Surface Methodology (RSM) and Central Composite Designs (CCD), the influence of independent process variables, such as soy lecithin, cholesterol content and surfactant concentration, on dependent variables, such as entrapment effectiveness and vesicle size of naproxen transfersomes, was assessed. In vitro, ex-vivo, and in vivo drug release of formulations were also studied.

Results: It was discovered that the NTG7 formulation of transfersomes had the maximum entrapment effectiveness and ideal vesicle diameter. The optimized NTG7 formulation displayed a maximum drug content of 97.4% and a maximum drug release of 88.03%. The release of naproxen from the final gel adhered to the Korsmeyer-Peppas release model. The ex-vivo drug release of the optimized formulation was found to be 85.91% for 24 h. The maximum drug concentration after oral administration was 843.54±7.67ng/ml, and T_max was 3.0±0.08h. The improved formulation's AUC_0-∞was greater than the commercial formulation's. A higher drug concentration in the blood compared to the marketed formulation suggested better systemic absorption of naproxen from the gel formulation. After three months, at a temperature range of 2 to 8 °C, the formulation demonstrated correct semisolid consistency and good stability and there was also no appreciable change in the initial values of appearance, pH, and % drug content.

Conclusion: The above findings imply that the gel created using naproxen-loaded transfersomes may be a potentially valuable new formulation.

QUALITY BY DESIGN SUPPORTED CONSTRUCTION OF ORAL FAST-DISSOLVING FILMS FOR TELMISARTAN: RECONNOITERING THE QUALITY ATTRIBUTES

2023-12-12T10:53:59+0530

Objective: The angiotensin II receptor antagonist telmisartan (TMS) is often used to treat hypertension. The BCS class II antihypertensive drug TMS has a low solubility, poorly absorbed when taken orally. The goal of this study was to formulate an oral fast-dissolving film (OFDF) of TMS. In recent years, the concept of a rapidly dissolving dosage form as an innovative delivery system has gained popularity. By decreasing dosing frequency, maximize therapeutic effectiveness, bioavailability, and stability. It will also prevent the drugs from being metabolized in the first place. This technique allows for faster drug absorption from the gastrointestinal tract (GIT), which might result in a more rapid onset of action.

Methods: An experimental design known as Box-Behnken was employed to optimize a OFDF. Mango kernel (100-300 mg), maltodextrin (200-350 mg), and propylene glycol (PG) (15-30%) were chosen as independent variables with the highest preference. Included measurements of T5 tensile strength, disintegration time, folding endurance, elongation, and drug release efficiency as dependent variables.

Results: The physical properties of the films were found to be satisfactory, and Fourier transform infrared (FTIR) analysis failed to detect any drug-polymer interaction. F4 was found to have the greatest bioadhesive strength of 49.82 gm and the longest ex-vivo mucoadhesion duration of 189 min. A higher concentration of mango kernel in the formulation resulted in a greater rate of drug release. More than 60% of the drug was discharged within 10 min.

Conclusion: The oral mucosa of a rat was used for ex-vivo for irritation studies. Based on the pharmacokinetic plasma parameters, which is made into quick-dissolving films that are taken by mouth, is much better absorbed than aqueous suspensions. Studies of the enhanced formulation's stability showed that F4 may be stored for up to three months without deterioration.

PREPARATION, CHARACTERIZATION AND EVALUATION OF GELLAN GUM/GLYCOL CHITOSAN BASED BAICALEIN HYDROGEL FOR WOUND HEALING

2023-10-19T16:36:24+0530

Objective: The present work was emphasized on preparation, characterization and evaluation of baicalein loaded hydrogel to promote healing of wounds.

Methods: Baicalein loaded hydrogel was developed using Gellan gum and Glycol chitosan polymers. Prepared hydrogels were characterized for various parameters like Field Emission Scanning Electron Microscopy (FE-SEM), swelling property, entrapment efficiency, rheology and drug release. Wound healing study was investigated by using incision dead space wound models. Healing effect was assessed by measurement of tensile strength, collagen content, hydroxyproline content, protein content and antioxidant status.

Results: The percent entrapment efficiency of optimized hydrogel found to be 89.78±2.07 which resulted in controlled release of drug 85.03% in 12 h. The significant increased level of catalase and superoxide dismutase (SOD) was noticed in dead space wound model. The tensile strength study shows increase in collagen synthesis due to treatment with Baicalein loaded hydrogel. The higher collagen content, better granulation, increase in tensile strength was noticed. Histopathological examination also confirmed higher degree of re-epithelialization and enhanced cutaneous wound repair.

Conclusion: In conclusion, biodegradable Baicalein loaded hydrogel might have high potential for wound healing with improved oxidative status and extended release of Baicalein.

THE NEW APPROACHES TO IDENTIFICATION OF TINCTURES AND MEDICINAL PLANTS

2023-11-13T14:12:12+0530

Objective: The objective of this study is to develop methods for identifying herbal medicines and tinctures by processing spectral results across a wide range of wavelengths using principal component analysis (PCA).

Methods: Medicinal plants and tinctures of valerian, motherwort, and hawthorn have been analyzed using UV spectrophotometry, spectrofluorimetry, ATR FTIR spectrometry, and X-ray fluorescence spectrometry. PCA was used to process the results of spectral analysis. Statistical processing of spectral results was carried out using the OriginPro program (OriginLab Corporation, USA, 2021).

Results: For herbal medicines with sedative, hypotensive, and cardiotonic effects, spectral data libraries have been created in the following dimensions: UV spectrophotometry with 1800 absorption units (A_i), spectrofluorimetry with 4010 fluorescence intensity units (I_i), IR spectroscopy with a light transmittance of 50250 units (T_i), and X-ray fluorescence spectrometry with an intensity of 1568 (I_i). These libraries were used as the primary matrices for PCA. Visualization of the PCA results was done using a scores plot and a loadings plot, which illustrate the contribution of each principal component (PC) to the PCA model. After performing chemometric processing on the original spectral results, it was discovered that samples belonging to the same botanical genus occupy distinct and compact regions in two-dimensional or three-dimensional space. Unknown plant samples (blind samples) and samples of other botanical species were successfully tested using new method.

Conclusion: For the first time, tinctures and medicinal plants were identified based on their botanical genus using spectral techniques coupled with principal component analysis, eliminating the need for a chemical reference substance.

MOLECULAR DOCKING OF THE KERUING's (DIPTEROCARPUS) GENUS, SECONDARY METABOLITES OF THE DIPTEROCARPACEAE FAMILY'S AS ANTI-INFLAMMATION AGAINST CYCLOOXYGENASE-2 (COX-2)

2023-11-10T09:18:49+0530

Objective: Kalimantan, Indonesia, has a tropical forest abundant in forest products. One of these products is the Dipterocarp tree, which includes the Keruing genus (Dipterocarpus). Dipterocarpus contains secondary metabolites that may be potential sources for new drug compounds. One of these metabolites has the potential to act as an anti-inflammatory agent. Based on pharmacophore modelling and molecular docking, this study used molecular docking to investigate the inhibitory mechanism and affinity of Dipterocarpus secondary metabolites on the 3N8Y inflammatory receptor.

Methods: The study involved multiple stages, such as preparing and optimizing the structure of the test compounds, constructing a 3D receptor structure of 3N8Y, validating the methodology, and performing energy docking simulations to analyze the interactions. From the study that has been done, the results for the test compounds were evaluated for their MolDockScore, Pharmacokinetic parameters (ADME), and toxicity.

Results: The results revealed that the oligomer resveratrol compound exhibited the lowest MolDockScore value of-104.7400, comparable to natural ligands. In addition to that, this method produces reliable outcomes through pharmacokinetic predictions such as HIA (88.4794%), Caco2 (5.1917 nm/sec), and PPB (100%). Furthermore, the toxicity profile exhibited negative results for mutagenic, non-mutagenic, and carcinogenic tests, including genotoxic and nongenotoxic substances.

Conclusion: The oligomeric resveratrol (3',5',4-trihidroksi-trans-stilben) compounds have potential as anti-inflammatory agents by acting on the 3N8Y receptor, which further needs to be tested in vivo.

FORMULATION, CHARACTERIZATION AND OPTIMIZATION OF FOLIC ACID-TAILORED DAIDZEIN SOLID LIPID NANOPARTICLES FOR THE IMPROVED CYTOTOXICITY AGAINST COLON CANCER CELLS

2023-11-17T12:36:28+0530

Objective: The study aims to formulate and optimize daidzein-conjugated folic acid solid lipid nanoparticles (DZN-FA SLNs) to improve bioavailability and target site specificity for the treatment of colon cancer, a significant global health concern associated with high morbidity and mortality.

Methods: DZN-FA SLNs were prepared using the microemulsion method. They were prepared and optimized using design expert software. Physicochemical characterization like differential light scattering (DLS), Fourier transformed infrared spectroscopy (FTIR), scanning electron microscope (SEM), In vitro drug release and In vitro cell line studies and accelerated stability studies were carried out in the optimized batch formulation.

Results: The results indicated that particle size for optimized DZN-FA SLNs was in the range of 212 to 620 nm, zeta potential of-20 mV, drug entrapment efficiency of 72%. In vitro drug release for the prepared formulation showed 53% over 48 h.

Conclusion: The optimized DZN-FA SLNs could aid in a better formulation targeting colon cancer cells, thereby reducing systemic effects. The optimized DZN-FA SLNs have demonstrated excellent inhibitory properties on Caco-2 cells, with an IC₅₀ value of 10 µg/ml, offering a promising innovation in cancer treatment by providing targeted and effective therapy for colon cancer while minimizing the impact on normal cells.

FORMULATION AND EVALUATION OF MODIFIED PULSATILE CAPSULE FOR CHRONOPHARMACOTHERAPY OF RHEUMATOID ARTHRITIC PAIN

2023-08-07T15:03:58+0530

Objective: The objective of the present study was to design and evaluate pulsincap system for chrono pharmacotherapy of rheumatoid arthritis that combines advantages of both immediate and sustained release technology with the suitable delay of drug release.

Methods: Pulsatile drug delivery system based on pulsincap® technology was designed using mucoadhesive microspheres and Tramadol bilayer tablet plugs. The drug-excipient interaction was carried out by FTIR. Hardness, thickness, lag time, and swelling index all play a role in optimizing tablet plugs. The microspheres were examined for parameters such as particle size, surface morphology, encapsulation efficiency, swelling index, % mucoadhesion, and in vitro dissolution.

Results: In modified pulsincaps, bilayer tablet plug shows drug release within 40 min and hydrogel plugs shows good swelling index and suitable lag time. In microspheres formulations, MF9 is the most suitable among them as it shows better drug content, particle size, surface morphology, in vitro drug release, and release kinetics. The drug is released right away, followed by the dissolution of the enteric coating at pH 6.8, followed by a suitable delay of 6 hours, and then the maximum amount of drug release is 99.62% at the end of 10^thh.

Conclusion: The pulsatile delivery system developed with HPMCK4M and tamarindus gum as plugging material showed a satisfactory lag period when compared to Tamarindus gum alone. Drug release can be achieved from treated gelatin capsule and hydrogel plug for a prolonged period by MF9 formulation.

NEURAL NETWORK-BASED ADVERSE DRUG REACTION PREDICTION USING MOLECULAR SUBSTRUCTURE ANALYSES

2023-11-23T12:16:27+0530

Objective: This study aims to enhance early detection and prediction by exploiting drug molecular substructures, overcoming challenges posed by limited authentic patient data in the medical domain.

Methods: The study implemented a neural network approach to optimize molecular fingerprint algorithms and employed various machine learning algorithms for predictions. Additionally, the study identified and extracted substructures associated with severe Adverse Drug Reactions (ADRs), validating their presence within drug structures through a comparison with a random set of drug structures. Predictions were made for specific molecular structures, and results were validated using clinical evidence from the literature.

Results: Optimized molecular fingerprint algorithms and diverse machine-learning models yielded promising outcomes. The Area Under Curve (AUC) value for the fingerprint dataset was obtained at approximately 65%, and integrating it with patient data significantly improved the performance by about 30%. Substructure analysis pinpointed key components linked to severe ADRs, reinforcing the predictive prowess of the model. Predictions for specific molecular structures were corroborated using clinical evidence from the literature, fortifying the credibility of the proposed approach.

Conclusion: In conclusion, this research effectively tackles challenges in the early detection and prediction of ADRs by leveraging machine learning algorithms, focusing on drug molecular substructures. The optimized model, incorporating both fingerprint and patient datasets, demonstrated significant improvements in predictive performance. Identifying and validating substructures linked to severe ADRs contribute to the model's reliability. The study's findings are vital for advancing drug safety and laying the groundwork for further strides in predictive modeling within the medical domain.

EFFECT OF PEGYLATED POLYPROPYLENE IMINE DENDRITIC ARCHITECTURE ON PHARMACOKINETICS OF PYRAZINAMIDE ON RABBITS

2023-10-07T15:37:58+0530

Objective: This study sought to investigate the impact of pegylated polypropylene imine dendrimer-loaded pyrazinamide on drug delivery and assess this novel formulation's pharmacokinetic parameters.

Methods: Various concentrations of pyrazinamide-loaded dendrimers were formulated in four distinct batches, with the most promising formulation selected for administration to New Zealand rabbits. Plasma concentrations of the drug were subsequently compared to those of the pure drug. Pharmacokinetic parameters, including maximum plasma concentration (C_max), time to reach C_max (t_max), the area under the curve (AUC), the area under the first moment curve (AUMC), elimination rate constant (λz), biological half-life (t_1/2), and mean residence time (MRT), were meticulously determined.

Results: The plasma drug concentration Vs time profile illustrated a sustained release pattern for the pyrazinamide drug-loaded dendrimer formulation compared to the pure drug. While a minor alteration was observed in peak plasma concentration, a notable divergence was noted in all other pharmacokinetic parameters. The AUC demonstrated a fourfold increase for pyrazinamide drug-loaded dendrimers, rising from 8657.94±295.10 to 34663.89±702.89 (ng/ml/h), and the mean residence time nearly doubled when compared to the pure drug.

Conclusion: Pyrazinamide drug-loaded dendrimers exhibit significant potential for enhancing drug release compared to the pure drug. This novel formulation promises a substantial and sustained drug release profile, holding promise for improving therapeutic outcomes and patient compliance in the treatment of relevant conditions.

A RELIABLE RP-UPLC-TUV METHOD FOR SIMULTANEOUS ESTIMATION OF CLARITHROMYCIN, AMOXICILLIN, AND VONOPRAZAN IN CO-PACKED PHARMACEUTICAL DOSAGE FORMS: METHOD DEVELOPMENT AND VALIDATION WITH STABILITY INDICATING PROPERTIES

2023-12-06T06:50:50+0530

Objective: The study aims to develop a reliable RP-UPLC-TUV method for simultaneous estimation of Clarithromycin, Amoxicillin, and Vonoprazan in bulk and combined dosage.

Methods: A simple, specific, and reliable method for determining Clarithromycin, Amoxicillin, and Vonoprazan has been developed using the RP-UPLC method. In order to successfully separate Clarithromycin, Amoxicillin, and Vonoprazan, 1.0 µl of a 100 % level solution was injected into a Hibar C18 (100 x 2.1 mm and 2 µm) column. The mobile phase consisted of Ammonium Acetate and Acetonitrile in equal volumes, and the flow rate was kept at 0.3 ml/min while the detection wavelength was set to 210 nm. Both the column and the injection port were kept at a temperature of 30 °C at all times.

Results: The retention time (RT) of Clarithromycin, Amoxicillin, and Vonoprazan was observed at 1.24 min, 0.97 min and 1.66 min, correspondingly with accepted system suitability. The linear responses were observed for Clarithromycin, Amoxicillin, and Vonoprazan in the range of 25 to 150 µg/ml, 25 to 150 µg/ml and 1 to 6 µg/ml, respectively. The LOD and LOQ values were calculated to 0.07 µg/ml and 0.22 µg/ml for Clarithromycin, 0.81 µg/ml and 2.45 µg/ml for Amoxicillin and 0.03 µg/ml and 0.09 µg/ml for Vonoprazan. The % RSD values of both precision were assessed in the range of 0.8-1.4. The mean recovery of Clarithromycin, Amoxicillin, and Vonoprazan was in the range of 99.66 %-100.88 %. The statistical analysis of the validation parameters confirmed that the approach was reliable in terms of its accuracy, sensitivity, and precision while also exhibiting a high degree of sensitivity. The study of analytes in a variety of stressful situations guarantees the stability of the substances, ensuring that they represent the method's stability indication.

Conclusion: The newly established technique is quite effective in separating Clarithromycin, Amoxicillin, and Vonoprazan from one another. Also separated with excellent resolution were the degradation products that were formed as a result of the stress conditions. The study concluded that the developed method has considerable adoption in the pharmaceutical sector.

ISOLATION AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES FROM CRAB SHELL WASTE (PORTUNUS PELAGICUS)

2023-10-20T16:36:17+0530

Objective: The purpose of this study was to isolate and characterize of chitosan nanoparticles derived from Portunus pelagicus shell waste.

Methods: Chitosan was isolated by deproteination, demineralization, and deacetylation methods. Furthermore, nanoparticles (NPs) were made by the ionic gelation method by dissolving chitosan in a mixture of acetic acid and sodium tripolyphosphate. The particle size analyzer and Fourier Transform Infrared Spectroscopy were used to measure the particle size of NPs and determine the functional group and degree of deacetylation.

Results: The yield percentage of chitosan was 90.7%. The size of chitosan nanoparticles based on the highest intensity is 15.05 nm with a polydispersity index (PDI) value of 0.1140 at a concentration of 1%. Based on the degree of deacetylation of chitosan nanoparticles, it was found to be 84.98% at 1% concentration.

Conclusion: The conclusion of this study is the formation of chitosan nanoparticles (1-100 nm) isolated from Portunus pelagicus shell waste. Based on the degree of deacetylation, chitosan nanoparticles with high chitosan content (>75%) were obtained.

ENHANCING THE PHYSICAL CHARACTERISTICS AND SHELF LIFE OF RICE WATER (ORYZA SATIVA L.) GEL SHAMPOO: THE ROLE OF PROPYLENE GLYCOL CONCENTRATION

2023-11-01T11:33:03+0530

Objective: This study aims to determine the effect of variations in propylene glycol concentration on the physical properties and physical stability of rice water shampoo gel and the physical strength of rice water shampoo gel preparation.

Methods: The active ingredient was rice water, which was prepared by washing rice with water at the proportion of 1:1. The rice water then was applied to HPMC K4M-based gel preparations and further designed to prepare shampoo gel with varying concentrations of propylene glycol 8%, 10%, and 12%. The rice water shampoo gel was evaluated for its organoleptic properties, pH, viscosity, spreadability, flowability test, softness test, and physical stability test.

Results: The results of the physical properties test on the three formulas produced an organoleptic clear pale yellow color, lemon odor, and semi-solid shape. The pH test results obtained by F1 was 7.24±0.08, F2 was 5.89±0.01, and F3 was 6.02±0.01. The viscosity test results obtained by F1 amounted to 2082±80.07 cP, F2 amounted to 4987±883.88 cP, and F3 amounted to 6531±232.79 cP. The foam height test results obtained by F1 amounted to 4.6±2.11 cm, F2 amounted to 1.46±0.05 cm, and F3 amounted to 1.7±0.17 cm. Variations in propylene glycol levels affect the physical properties of shampoo gel preparations at pH, viscosity, and foam height but do not affect the organoleptic practice. The stability test that was conducted at weeks 0, 1, 2, 3, and 4 with varying levels of propylene glycol showed significant changes on viscosity and foam height stability.

Conclusion: Variations in the concentrations of propylene glycol in the three formulations affect the physical but have no effects on the pH stability of the rice water shampoo gel preparation.

ADVANCEMENTS IN MICRONEEDLE TECHNOLOGY: COMPREHENSIVE INSIGHTS INTO VERSATILE DRUG DELIVERY MECHANISMS

2023-10-08T17:26:26+0530

Microneedle-based transdermal medication administration is a revolutionary drug delivery technique that has advantages over parenteral and oral drug delivery systems. They are convenient, painless, safe, and effective. Due to the skin’s stratum corneum layer, the majority of drugs only have a limited impact, which constitutes a thickness of about 10 to 15 µm and acts as a barrier for molecules to reach the site of action, allowing just a few molecules to pass through. To overcome this, many researchers have concentrated on using microneedles to bypass the stratum corneum barrier. The main goal of microneedles is to get the drug into the epidermis without disrupting nerve endings. Micron-sized channels created by the skin layer being broken by microneedles transport the medication directly to the epidermis or higher dermis, avoiding the barrier layer and into the systemic circulation. As a result, the microneedle can improve transdermal drug delivery. Microneedles are fabricated in different forms, such as “Solid Microneedles,” “Coated Microneedles,” “Dissolving or Biodegradable Microneedles,” “Hollow Microneedles” and Hydrogel-forming Microneedles, through the use of components including polymers, polysaccharides, silicon, and metals. Micromolding, laser cutting, dip coating, 3D printing and its techniques are just a few of the processes used to make microneedles. Recently, microneedles have become popular for delivering drugs, genes, proteins, RNA and vaccines, demonstrating significant therapeutic effects. A variety of nano-carriers, along with different delivery methods, assist in emphasizing the use of microneedles in the meantime.

A REVIEW ON DEVELOPMENT OF COLON TARGETED DRUG DELIVERY SYSTEM

2023-09-11T18:54:46+0530

The purpose of this review was to select a promising drug delivery system for colon diseases. This review covers the development of Colon Targeted Drug Delivery System (CTDDS) using 36 y (1986-2022) data from various research and review articles. All fig. designed using by BioRender website. vThe colon-targeted drug delivery systems developed for the specific site drug delivery which applied for both local and systemic actions of the drug; since the drug targeted to be release within the colon, the unwanted systemic side effects are reduced along with it. Systemic side effects include organ damage, respiratory diseases and, cardiovascular damage and other illnesses. Colon-targeted drug delivery system used in the treatment of diseases in the colon, including ulcerative colitis, irritable bowel syndrome and colorectal cancer. The benefit of colon-targeted drug delivery besides the reduction of side effects also include protection from premature drug release or burst in the stomach or small intestine before reaching the colon. For the development of drugs with such benefits and advantages, drug delivery systems and approaches have used for Colon targeted drug delivery systems, varying from conventional colon-targeting drug delivery systems to novel approaches for Colon-targeted drug delivery systems. Conventional drug delivery includes the use of prodrugs, pH-dependent, time-dependent, matrix-based systems, polysaccharides-derived systems, and bio-adhesive system while novel approaches include types such as port system, pulsincap system, pressure-controlled system, osmotic controlled system, CODES, and the newest approach wish is the use of nanotechnology in colon targeted drug delivery. In this research both techniques reviewed, and their types discussed as well. The limitation of their uses and the advantage of each system discussed with a breakdown of the different mechanisms used to formulate such systems. A successful colon targeting delivery can release the drug to a specific segment in colon due to presence of different colonic enzymes formed by microorganisms that metabolize drug carrier linkage. Use of combined approaches i.e., conventional systems and newer approaches may be the best way to cure colon diseases using an optimized colon drug delivery system.

A REVIEW ON RECENT ADVANCES IN TRANSDERMAL DRUG DELIVERY SYSTEMS OF TAMSULOSIN

2023-11-27T13:22:02+0530

Tamsulosin is a highly selective α1-adrenoreceptor antagonist. It has been developed to treat signs and symptoms of benign prostatic hyperplasia. Tamsulosin is absorbed quickly and completely in intestinal mucosa and is eliminated gradually after oral administration, which might generate some side effects as postural hypotension in number of patients. Transdermal drug delivery systems were developed for prolonged tamsulosin delivery in order to control its bioavailability and minimize its side effects. Hence, the present review aims to discuss thoroughly the various transdermal drug delivery systems of tamsulosin investigated in recent years. This review also discusses the skin as a route of drug administration, technologies in transdermal drug delivery along with different techniques used in the preparation of transdermal delivery systems of tamsulosin and their effects on its release and permeation.

BIOSURFACTANTS: SUSTAINABLE ALTERNATIVE TO SYNTHETIC SURFACTANTS AND THEIR APPLICATIONS

2023-12-06T15:15:30+0530

Biosurfactants are surface active agents produced by microorganisms, which help reduce surface or interfacial tension between two immiscible liquids like oil and water. In recent years, Due to their environmentally friendly nature and wide range of applications in various industries, they can act as a sustainable alternative to synthetic surfactants. This review article provides an overview of biosurfactants, emphasizing their need for biosurfactants, the production process, and their classification based on molecular weight, charge, and the microorganism they derived. The advantages include biodegradability, biocompatibility, low toxicity, surface activity, and specificity, and various areas where the biosurfactant used are emulsification, thermal stability, pH stability, wetting ability, foaming ability, and spreadability. Research on using biosurfactants in various formulations like nanoparticles, liposomes, transdermal application, nanoemulsion, and nanocapsules is also highlighted in this review to support its application in the medical field. Biosurfactants are also utilized in various fields like the pharmaceuticals, cosmetics, food, and oil industries. However, they have their drawbacks, which include high production costs, variability in production yield, sensitivity to the environment, lack of standardization, hurdles in regulatory approval, and research and development limitations. Despite certain drawbacks, biosurfactant offers a sustainable alternative to synthetic surfactants.

A SYSTEMATIC REVIEW: EXPLORATION OF PROCESS ANALYTICAL TECHNOLOGY TECHNIQUES (PAT) AND THEIR MULTIFACETED ADVANTAGES IN INDUSTRIAL PROCESSES

2023-11-01T22:12:58+0530

FDA initiated the PAT technology framework in the year of 2004 with the guidelines of “A framework of innovative pharmaceutical development, manufacturing and quality assurance. With that, the International Council for Harmonisation has also initiated continuous process verification to overcome the limitations of traditional methods and improve the understanding of the process and quality of the product throughout the product lifecycle. Since the year of implementation, the advancement of analytical and chemometric tools has evolved to deliver consistent quality products by understanding their process and product performance. However, the pharmaceutical industry was lacking in this technicality and implementation of highly regulated specifications. To this respect, we have stated some of the PAT tools, including NIR, Raman and Terahertz spectroscopy, as they will transfer to the futuristic prospects of analyzing the drug product with non-destructive, improved process understanding, real-time monitoring, and enhanced data integrity. This review article emphasizes the importance of PAT technology with different monitoring processes with their historical background and regulatory framework. Special attention was given to strategies, challenges, opportunities, and the compatibility of PAT tools with data fusion. Further, this will give a high-priority disciplinary scientific topic to Pharma 4.0.

REVOLUTIONIZING DRUG DELIVERY INNOVATION: LEVERAGING AI-DRIVEN CHATBOTS FOR ENHANCED EFFICIENCY

2023-12-19T13:54:29+0530

This study aims to delineate the pivotal role of ChatGPT, an Artificial intelligence-driven (AI) language model, in revolutionizing drug delivery research within the pharmaceutical sciences domain. The investigation adopted a structured approach involving systematic literature exploration across databases such as PubMed, ScienceDirect, IEEE Xplore, and Google Scholar. A selection criterion emphasizing peer-reviewed articles, conference proceedings, patents, and seminal texts highlights the integration of AI-driven chatbots, specifically ChatGPT, into various facets of drug delivery research and development. ChatGPT exhibits multifaceted contributions to drug delivery innovation, streamlining drug formulation optimization, predictive modeling, regulatory compliance, and fostering patient-centric approaches. Real-world case studies have underscored its efficacy in expediting drug development timelines and enhancing research efficiency. This paper delves into the diverse applications of ChatGPT, showcasing its potential across drug delivery systems. It elucidates its capabilities in accelerating research phases, facilitating formulation development, predictive modeling for efficacy and safety, and simplifying regulatory compliance. This discussion outlines the transformative impact of ChatGPT in reshaping drug delivery methodologies. In conclusion, ChatGPT, an AI-driven chatbot, has emerged as a transformative tool in pharmaceutical research. Their integration expedites drug development pipelines, ensures effective drug delivery solutions, and augments healthcare advancements. Embracing AI tools such as ChatGPT has become pivotal in evolving drug delivery methodologies for global patient welfare.