Int J App Pharm, Vol 15, Issue 1, 2023, 227-233Original Article
OPTIMIZATION, FORMULATION AND CHARACTERIZATION OF NANO BASED TDDS OF EPLERENONE
SHINDE RAMESH VITHOBA, MALARKODI VELRAJ*
Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies, Chennai, Tamil Nadu, India, Chennai, Tamilnadu, India
*Email: malarkodisanna@gmail.com
Received: 04 Jun 2022, Revised and Accepted: 15 Oct 2022
ABSTRACT
Objective: The proposed work was aimed to formulation, characterization and optimization of transdermal patches of nanoparticles of eplerenone for efficient transdermal delivery of the drug.
Methods: Eplerenone nanoparticles transdermal patches were formulated by the casting evaporation method. Transdermal patches were made using combinations of hydroxypropyl methylcellulose (HPMC), Eudragit RS 100. Physical characterization evaluation (organoleptic properties, pH, weight uniformity, thickness uniformity, percent moisture content, and tensile strength) was then performed. The permeation of eplerenone nanoparticles into the skin was evaluated using Franz diffusion cell.
Results: Eplerenone nanoparticles transdermal patches could be formulated by the casting evaporation method with the thickness of the patches ranged from 0.10±0.11 mm to 0.15±0.54 mm. The average weight of the patches 4 cm2 patches ranged from 350±0.202 mg to 386±0.527 mg, and the percent moisture content ranged from 1.0 to 6.0%. Folding endurance of prepared patches was in the range of 355±0.20 to 368±0.20. Prepared batches NS1 to NS9 evaluated for percentage moisture uptake and loss as well as for pH measurement. The result of in vitro drug release study for batch NS9 containing 30 %/cm 2/h and 87.74 % released in 16 h.
Conclusion: All patches met the requirement of the physical characterization for the transdermal patch.
Keywords: TDDS, Eplerenone nanoparticle, ERS 100, Transdermal matrix
© 2023 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open-access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
DOI: https://dx.doi.org/10.22159/ijap.2023v15i1.45433. Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
The skin is one of the most extensive organs of the human body. This multi-layered organ receives approximately one-third of all blood circulating through body. With a thickness of about a millimetre, the skin separates the underlying blood circulation network from the outside environment. Skin permeation kinetics is vital to the successful development of transdermal therapeutic system. Transdermal drug delivery systems (TDDS) are dosage forms involve drug transport to viable epidermal and or dermal tissues of the skin for local therapeutic effect while a very major fraction of the drug is transported into the systemic blood circulation [1]. Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels does not overcome the effects of eplerenone [2].
The use of nano-formulations has emerged as a potential suggests keeping away from barriers related with transdermal therapy [3]. Due to the merits of small particle size, higher drug retention, alongside with their targeting ability, nano-formulations have been regarded best TDDSs. Accordingly, many strategies have been adopted to enhance the transdermal delivery of bioactive agents using nanoparticulate drug delivery systems, such as lipo-some, transferosomes, ethosomes, dendrimers and microemulsions. Liposomes as one of the transdermal delivery systems, have been studied due to the fact that the 1980s and have attracted a lot of interest. Nevertheless, liposomes do no longer penetrate deeply into the skin of rats and are restrained to the higher layer of the skin. By contrast, transferosomes, ultra-flexible liposomes, signify a promising lipid-based vesicular system that is significantly exploited in the area of transdermal drug delivery. As an end result of their ultra-flexible membrane characters, they have the potential to deliver the drug both into or via the skin, relying on the application, with excessive efficacy. The vesicular transferosomes are greater elastic than different vesicular delivery systems, such as liposomes, and are accordingly properly appropriate for skin penetration [4, 5]. The proposed work was aimed to optimization the formulation and characterization of transdermal patches of eplerenone for efficient transdermal delivery of the drug in the pharmaceutical system to enhance the antihypertensive effect of eplerenone.
MATERIALS AND METHODS
Materials
Eplerenone were taken from the Chemo Pvt Ltd, Mumbai, Eplerenone nanoparticles were formulated from hydroxypropyl methylcellulose (HPMC), Eudragit RS 100, Other materials included HPMC (LOBA Chemie Pvt. Ltd., Mumbai, India), Eudragit RS 100 (Chemdyes corporation, Rajkot, India), Eudragit RL 100 (Chemdyes corporation, Rajkot, India), Propylene glycol (Chemdyes corporation, Rajkot, India), PEG 400 (Chemdyes corporation, Rajkot, India), ethanol (Shree chalthan vibhag khand udyog sahkari mandli Ltd, Surat).
Top-down syntheses
In this strategy, destructive methodology is utilized. Beginning from bigger particle, which deteriorated into littler units and afterward, these units are changed over into reasonable NPs. Instances of this technique are crushing/grinding. The processing technique was utilized for this reason and the drug powders were finely processed for various time frames with the assistance of artistic balls and a notable planetary plant [6]. They demonstrated the impact of processing time on the general size of the NPs through various portrayal strategies and characterized their surface morphology and size by the SEM, TEM and zeta potential [7].
Differential scanning calorimetry
The DSC of the eplerenone nanoparticle was recorded by a differential scanning calorimeter equipped with a computerized data station. The DSC measurements were performed on a DSC 60, Shimadzu, Japan instrument. Accurately weighed sample were placed in sealed aluminium pans before heating under nitrogen flow (20 ml/min) at a scanning rate of 100c/min [8]. An empty aluminium pan was used as a reference. Melting point was determined for the identification of drug nanoparticle [9].
Scanning electron microscopy
Scanning electron microscopy of drug nanoparticles was carried to determine the external morphology. The sample was mounted directly onto the SEM sample holder using double-sided sticking tape and images were recorded at the required magnification at an acceleration voltage of 20 kV using a scanning electron microscope [10, 11].
Dose for the formulation of transdermal matrix patch of eplerenone
Diameter of Petri plate =6.8 cm,
Area of Petri plate = 3.14 × (3.4)2 = 36.29 cm2
Area of patch = 2 cm × 2 cm = 4 cm2
Total no. of patches in each Petri plate = Area of Petri plate/Area of patch=36.29/6= 6.04
Now, one patch contains 8 mg of the drug, then 6.04 patches contain 48.33 mg of the drug (49 mg).
Table 1: Formulation of nano-size eplerenone loading factorial design batches NS1 to NS9
| Batch code | NS1 | NS2 | NS3 | NS4 | NS5 | NS6 | NS7 | NS8 | NS9 |
| Eplerenone (mg) | 49 | 49 | 49 | 49 | 49 | 49 | 49 | 49 | 49 |
| ERS 100(mg) | 250 | 250 | 250 | 225 | 225 | 225 | 200 | 200 | 200 |
| HPMC K15(mg) | 50 | 50 | 50 | 75 | 75 | 75 | 100 | 100 | 100 |
| Water (ml) | 11 | 11 | 11 | 11 | 11 | 11 | 11 | 11 | 11 |
| Ethanol (ml) | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 |
| PG (%) w/w of dry polymer Wt. | 20 | 20 | 20 | 20 | 20 | 20 | 20 | 20 | 20 |
| MO (%)w/w of dry polymer wt. | 10 | 20 | 30 | 10 | 20 | 30 | 10 | 20 | 30 |
Evaluation of Tdds
Thickness of the patch
The thickness of the medication stacked fix was estimated in various focuses by utilizing an micrometre screw gauge and decides the normal thickness and standard deviation for the equivalent to guarantee the thickness of the readied patch [12, 13].
Drug content
The amount of drug present in the patch was determined by dissolving the patch in 100 ml of phosphate buffer pH 6.8. At that point, the arrangement is to be separated through a channel medium and dissect the medication utilizing (UV method) at 245 nm [14, 15].
Percentage moisture content
The prepared patches were weighed exclusively and to be kept in a desiccator containing melded calcium chloride at room temperature for 24 h. After 24h the movies are to be rechecked and decide the rate dampness content from the beneath referenced formula [16].
……. (1)
Percentage moisture uptake
The weighted patches were kept in a desiccator at room temperature for 24 h containing a saturated solution of potassium chloride in order to maintain 84% RH. After 24 h the films are to be reweighed and determine the percentage moisture uptake from the below-mentioned formula [17].
……. (2)
Water vapor permeability
Glass vials of 5 ml capacity were washed thoroughly and dried to a constant weight in an oven. About 1g of fused Calcium chloride was taken in the vials and the polymer films were fixed over the brim with the help of an adhesive tape [18]. Then the vials were weighed and stored in a humidity chamber at 85 % RH condition for a period of 24 h. The vials were removed and weighed at various time intervals like 3, 6, 12, 18 and 24 h to note down the weight gain [19, 20].
Weight uniformity
The prepared patches were dried in an oven at 60° for 24 h before testing. A specified area of the patch is to be cut in different parts of the patch and weigh in digital balance. The average weight and standard deviation values are to be calculated from the individual weights [21].
Folding endurance
A strip of the specific area was cut evenly and repeatedly folded at the same place till it broke. The number of times the film could be folded at the same place without breaking gave the value of the folding endurance [22].
Percentage elongation break test
The percentage elongation break was determined by noting the length just before the breakpoint; the percentage elongation can be determined from the below-mentioned formula [23].
…… (3)
Where L1 is the final length of each strip and L2 is the initial length of each strip
Weight variation
The assessment of weight variation was performed by weighing individually drug-loaded five patches of every formulation on a digital balance. The average weights were calculated and the standard deviation from the average weights measured [24].
Tensile strength
Tensile strength of the prepared patches was measured by a privately collected instrument. The tensile strength of the patch was estimated utilizing a privately gathered instrument. In which one side of patch fixed into the iron screens and another side was associated with the paper holder where snare was embedded. One string was attached with this snare, which disregarded the pulley and a little dish appended to the opposite end for holding the weight. Little pointer was appended to the string, which goes over the scale attached on the base plate [25]. For estimation of tensile strength, patch was pulled and loads were bit by bit added to the dish to build the pulling power till the patch was broken. All out loads required to break the patch are considered as power, placing the estimation of power into the equation elasticity was measured. Tensile strength= × (+/). Where F is the power required to break; a, b, and L are the width, thickness and length of the patch individually and l is an extension of patch at the breakpoint [26].
Flatness
A transdermal patch ought to have a smooth surface and ought not choke with time. To assess this property flatness study was perform. In this study one segment of patch cut from the middle and two from each side. The length of each strip was estimated and a variety long note down. Zero percent narrowing will be proportionate to 100 percent flatness [27].
……. (4)
pH
Patch was set in a beaker and was soaked with 10 ml of distilled water and saved for 30 min. The pH was measure subsequent to bringing the terminal of the pH meter in contact with the outside of the plan and permit equilibrates for 2 to 3 min [28].
In vitro drug release studies
The in vitro release study was done with the semi-porous film utilizing Franz diffusion cell. The chamber comprises of two chambers, the giver and the receptor compartment. The giver compartment was open at the top and was presented to air [22]. The temperature was kept up at 37±0.5 ° C and the receptor compartment was furnished with testing port. The dispersion medium utilized was phosphate support (pH 7.4) [21].
RESULTS AND DISCUSSION
Table 2: Solubility study of eplerenone
| Medium solubility | Solubility | Calculated value |
| Ethanol | Freely soluble | 29 μg/ml |
| Methanol | Soluble | 24 μg/ml |
| Chloroform Soluble | Soluble | 19 μg/ml |
| Distilled Water | Practically insoluble | 7 μg/ml |
| pH 6.8 Buffer | Soluble | 21 μg/ml |
Solubility for eplerenone Nanoparticle proposed that uninhibitedly dissolvable in organic solvents, dissolvable in phosphate support pH 6.8 and for all intents and purposes insoluble in distilled water. In any case, a transdermal patch apply on the skin, in this manner to assess permeation of medication through skin pH, phosphate buffer pH 6.8 was select as a dispersion mode for additional investigation.
Table 3: The DSC test on eplerenone was presented below
| S. No. | Stage | Temperature |
| 1 | Onset | 198.22 °c |
| 2 | Peak | 198.25 °c |
| 3 | End set | 199.65 °c |
Fig. 1: Thermal analysis result of eplerenone nanoparticle
Fig. 2: Counter plot and (B) Response surface plot show the effect of polymer fixed weight ratio and mentha oil on the percent drug released in 1h from Batches NS1-NS9
Due to drug entrapment in the lipid, the melting point of eplerenone (pure drug) was 199.25 °C (fig. 1).
Analysis of variance and model equations for drug released in Q1(h)
For response surface analysis, a two-way analysis of variance was generated by Design Expert 9.0 software. The Model F-value was more than the tabulated F-value (3.56) which implies that the model is significant and the higher value of R2 (0.998) indicates good fitting of model. The polynomial equation derived for the estimation was mention below [15].
% CDR (16h) = 93.0956+3.63667* A+-1.55667* B+-0.07* AB+0.806667* A^2+-1.08333* B^2. …. Eq. (5)
32 Factorial Design in Design expert programme with Polynomial Quadratic Model and Multiple Linear Regression approach was used to optimize formulation and process parameters for nano-based transdermal patches formulation. The quadratic model suggests a P value of 0.0001 in the sum of squares. Selected the highest-order polynomial with significant additional terms and no aliasing. The chosen model has a minor lack of fit, as evidenced by the P-value of 0.0001 obtained from the Lack of Fit test. The Model F-value of 3.56 indicates that the model is statistically significant. An F-value of this magnitude has a 0.01 % chance of occurring due to noise. Model terms with P-values less than 0.05 are significant. The Adjusted R2 of 0.998 is reasonably close to the Predicted R2 of 0.9897; that is, the difference is less than 0.2. When all other factors are maintained constant, the coefficient estimate provides the expected change in response per unit change in factor value. In an orthogonal design, the intercept is the overall average response of all the runs. The coefficients are modifications based on the factor settings around that average.
The high levels of the factors are coded as+1 and the low levels of the factors are coded as-1 by default. By comparing the factor coefficients, the coded equation can be used to determine the relative impact of the components. It was discovered from the data that there was a good association between drug release (R2 = 0.9841), It determines whether there is an increase in polymer concentration (when using ANOVA) It exhibits P<0.0001. It could be because of the influence of lower concentration and higher plasticizer concentrations. P-value = 0.0001 was calculated using ANOVA.
Scanning electron micrographs (SEM)
The surface morphology of nanoparticles is another important parameter which influences the drug release and drug absorbance properties. The evaluation of the surface morphology of the prepared formulations was done by the help of SEM analysis. Examination of SEM images of the prepared nanoparticles revealed that these were spherical. SEM images of formulation were presented in fig. 3. The spherical shape of these nanoparticles is confirmed by the SEM analysis.
Fig. 3: Scanning electron micrographs of eplerenone nanoparticle
Aspect ratio
Aspect ratio was done for the nanoparticle sphericity for the flow property. Hot stage microscope was used for the measurement of the height and width of the nanoparticle. Aspect ratio was calculated from the following formula: From the above result aspect ratio of the nanoparticle was found to be 1.039. Guyot M. et al. has reported aspect ratio of the nanoparticle-based patches [14].
……………. (6)
Aspect ratio should be very near to 1 for the best spherical shape.
Partition coefficient
The log p estimation of eplerenone nanoparticle was 1.70, it was closer to standard worth. Log P value in a range of 1 to 4 indicates higher permeation through the skin.
Fig. 4: Aspect ratio of eplerenone nanoparticle
Transdermal patch for eplerenone was effectively arranged utilizing HPMC K15M and ERS 100 as a patch shaping polymers by dissolvable dissipation technique and last medication stacked patch was discover by formulation of examinations from the Arranged batch NS1 to NS9 were assess for various physiochemical parameter. After-effects of the physicochemical parameter of batches S1 to S9 speak to in table 7.2.6. Drug-loaded films (4 cm2) were weighing using Digital electronic balance Shimadzu, Japan. The weight of 4 cm2 patches ranged from 350±0.202 mg to 386±0.527 mg. In all the cases, the determined standard deviation esteems were low, which shows that the readied patches were uniform in weight, and along these lines, all the bunches passed the weight variety according to limits given in legitimate books. Acquired outcomes proposed that medication was consistently scattered in to polymeric scattering. With the assistance of a micrometer check, the thickness of fix was measure at six positions and the normal was note down. Prajapati ST et al. reported that the standard limits for the physicochemical evolution of the transdermal patches. [2] The result of batches NS1 to NS9 revealed that there were minor differences between the thicknesses of all the formulations; it was obtained in between 0.10±0.11 mm to 0.15±0.54 mm. Batch NS6 shows the highest thickness and NS4 shows the lowest thickness, this happens due to the different in polymer concentration and distribution difference over the Petri plate. Drug content of the transdermal patch was performed to find out the loading of the drug is uniform in the formulation or not. Folding endurance of prepared patches was in range of 355±0.20 to 368±0.20. Depending upon the concentration of propylene glycol and mentha oil, the results of folding endurance might be differed. Batches NS1 shows highest folding endurance with 368±0.20 indicates that the patches had sufficient mechanical strength and it would be remained as such during the treatment on the application site. The smoothness was measure manually for the prepared transdermal patch. An obtained result of the flatness study suggested that the length of the patch strip, before and after cuts was remain the same and it shows 2 to 3% constriction in all nine batches. Prepared batches NS1 to NS9 evaluated for percentage moisture uptake and loss as well as for pH measurement.
Table 4: Physicochemical evaluation of Eplerenone nanoparticle loading batches NS1-NS9
| Batch code | Weight variation (mg) | Thickness (mm) | Folding endurance | % Moisture uptake | % Moisture loss |
| NS1 | 369±0.527 | 0.12±0.04 | 368±0.20 | 1.63±0.04 | 1.56±0.59 |
| NS2 | 378±0.320 | 0.13±0.23 | 263±0.29 | 1.90±0.25 | 1.80±0.15 |
| NS3 | 369±0.527 | 0.12±0.12 | 356±0.23 | 2.40±0.18 | 1.96±0.68 |
| NS4 | 370±0.320 | 0.10±0.54 | 356±0.22 | 2.32±0.18 | 2.13±0.05 |
| NS5 | 386±0.527 | 0.14±0.24 | 364±0.24 | 1.93±0.35 | 1.46±0.09 |
| NS6 | 373±0.320 | 0.15±0.54 | 356±0.28 | 1.78±0.05 | 2.27±0.05 |
| NS7 | 373±0.324 | 0.13±0.11 | 355±0.20 | 1.63±0.01 | 2.55±0.32 |
| NS8 | 350±0.202 | 0.12±0.54 | 360±0.20 | 2.70±0.05 | 1.25±0.02 |
| NS9 | 351±0.301 | 0.10±0.74 | 355±0.62 | 1.56±0.64 | 1.84±0.69 |
(Where n = 3, mean±SD)
Ex-vivo skin permeation study of eplerenone nanoparticle
Plot of a combined measure of drug release versus time create for permeation contemplates and speak to in fig. 6. From this plot, permeation kinetic analysis, for example, penetration flux, permiability coefficient and enhancement proportion were determined. The outcomes uncovered that batch NS9 containing 30 %/cm2/hr and 87.74 % released in 16 h. Medication permeation improve with the higher grouping of SO because of the nearness of unsaturated fats, which change the structure of layer corneum and increment the dispersion of medication atoms through the various layers of the skin. Mittal A et al. reported that the diffusion coefficient of drugs in a PSA matrix is affected by the type of functional group of the drug. [15] The aftereffects of ex-vivo discharge likewise proposed that the concentration of SO and PG both had a significant impact on medicate discharge since unsaturated fats of SO improves the lipid dissolvability and PG improves water solvency by changing the extremity of fluid layer and improve solubilizing capacity for lipid particles. In this manner, consolidation of PG as a plasticizer in the medication stacked transdermal patches might be helpful for improving the physical quality just as drug release properties, thus use for achieving required medication permeability through the skin. The pace of medication release additionally relies upon choice of polymer and its conc. Medication release increments with increment in the convergence of the two polymers HPMC K15M and ERS 100 in light of the fact that hydrophilic nature of HPMC K15M and ERS 100 improve hydration and expanding property, which at last prompts swelling release in the introductory first hour. The arrival of medication from the polymeric framework happens as water enters inside the network, which makes the polymers swell, bringing about the controlled arrival of medication for a foreordained period. Anilreddy et al. showed an effect of the polymer concentration on the realease of the drug [7].
Table 5: Permeation kinetic parameters of batches NS1 to NS9
Batch code |
Transdermal flux Jss 2/h) |
Lag time (h) |
Permeability coefficient (Kp) (cm/h) | Diffusion coefficient (D) (cm/h×10-8) | Enhancement ratio |
| NS1 | 97.6±0.34 | 1.26±0.2 | 1.24×10-3±0.04 | 0.01236±0.05 | 1.234±0.01 |
| NS2 | 98.6±0.15 | 1.33±0.4 | 1.30×10-3±0.10 | 0.01390±0.18 | 1.235±0.02 |
| NS3 | 119.0±0.11 | 1.34±0.6 | 1.45×10-3±0.74 | 0.01472±0.17 | 1.337±0.03 |
| NS4 | 121.3±0.21 | 1.26±0.7 | 1.50×10-3±0.56 | 0.0158±0.14 | 1.339±0.04 |
| NS5 | 129.0±0.10 | 1.34±0.2 | 1.58×10-3±0.65 | 0.0159±0.14 | 1.436±0.03 |
| NS6 | 131.2±0.41 | 1.32±0.2 | 1.61×10-3±0.58 | 0.023±0.16 | 1.448±0.04 |
| NS7 | 137.6±0.20 | 1.37±0.1 | 1.72×10-3±0.65 | 0.025±0.10 | 1.548±0.06 |
| NS8 | 152.1±0.02 | 1.32±0.4 | 1.79×10-3±0.15 | 0.029±0.10 | 1.623±0.08 |
| NS9 | 164.4±0.04 | 1.33±0.4 | 1.90×10-3±0.16 | 0.0352±0.06 | 1.687±0.09 |
(Where n = 3, mean±SD)
Table 6: Kinetic models and regression coefficient
| S. No. | Equation | Regression coefficient |
| 1 | Zero-order | 0.9916 |
| 2 | First order | 0.5425 |
| 3 | Higuchi | 0.9752 |
| 4 | Korsmeyer-Peppas | 0. 9514 |
| 5 | Hixson Crowell | 0. 6803 |
Fig. 6: Comparative drug release profile of batches NS1-NS9
In ex-vivo drug delivery information of last chose optimized batch was exposed to various kinetic models to contemplate the instrument of medication discharge from the patch and through the skin. Gannu R. et al. reported a regression analysis of the nanoparticle based patch [27] Regression coefficient additionally recommended that medication discharge from the patch follow zero request and from the patch tranquilize was discharge ceaselessly in a controlled way up to 16 h. The correlation coefficient (R2) of Higuchi's model was seen as 0.9772 that shows diffusion of medication from the readied patches. In this manner, the chose batch NS9 followed zero order. Medication release component happen first by growing of polymer and drug was diffuse out from the matrix, so it follows Higuchi’s and Korsmeyer-Peppas model more effectively.
Stability study
The optimized batch NS9 exposed for stability studies as per ICH guidelines for 6 mo. The samples assessed for the drug content, folding endurance and ex vivo permeation study. The after-effect of this examination shows that the items have awesome steadiness at room temperature. Sharma S. et al. show effect of stability study on formulations [26] Consequences of ex vivo diffusion study, drug content and folding endurance likewise proposed that expansion in temperature measure of dampness in patch diminished because of this patch become brittle. Consequences of an improved batch uncovered that final formulation was steady at accelerated condition at 40±2 °C and 75±5 % RH. It uncovered that, readied patches stable and keeps up its physical respectability all through the investigation.
Table 7: Stability studies results of optimized batch NS9
| Stability conditions | Sampling time | Folding endurance | Drug content uniformity (%) | Ex-vivo drug release (%) |
| Accelerated condition (40±2oC and 75±5% RH) (Batch NS9) |
Initial (0 d) | 397±1.50 | 98.70±0.02 | 95.30±0.03 |
| After 15 d | 384±2.32 | 98.54±0.13 | 95.21±0.08 | |
| After 30 d | 371±1.02 | 98.21±0.10 | 94.19±0.15 | |
| After 90 d | 369±2.63 | 98.14±0.23 | 94.18±0.23 | |
| After 180 d | 364±2.04 | 98.02±0.51 | 94.07±0.14 |
(Where n = 3, mean±SD).
CONCLUSION
Eplerenone nanoparticles have been successfully formulated into transdermal patches using combinations of hydroxypropyl methylcellulose (HPMC), Eudragit RS 100 Physical characterization of Eplerenone nanoparticles transdermal patches showed the uniformity of Eplerenone nanoparticle transdermal patches. Eplerenone can be released from the transdermal patch and can be predicted that all eplerenone will be released in 16 h. eplerenone can penetrate into the skin and formulating eplerenone nanoparticles. Overall findings from this research show that the limitation of oral eplerenone administration can be solved by formulating eplerenone into eplerenone nanoparticles transdermal patches, especially for Antihypertensive therapy.
ACKNOWLEDGEMENT
The authors are grateful to VISTAS, Chennai, and Hon. Shri. Babanrao Pachpute Vichardhara Trust’s, Parikrama Group of Institutions, Kashti, for providing the required facilities for doing this work.
FUNDING
Nil
AUTHORS CONTRIBUTIONS
All the authors have equally contributed in this manuscript.
CONFLICT OF INTERESTS
No potential conflict of interest was declared by the authors.
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