ONE FACTOR RESPONSE SURFACE METHODOLOGY (RSM) FOR THE OPTIMIZATION OF ORAL VENLAFAXINE HCL CONTROLLED RELEASE ORGANOGEL

NISHANT OZA; AMI MAKWANA; TUSHAR A. GOHIL

doi:10.22159/ijap.2022v14i5.45517

Authors

NISHANT OZA C. U. Shah College of Pharmacy and Research, Wadhwan City 363030, Gujarat, India https://orcid.org/0000-0003-1840-3142
AMI MAKWANA C. U. Shah College of Pharmacy and Research, Wadhwan City 363030, Gujarat, India
TUSHAR A. GOHIL Smt. C. V. Gajera Pharmacy Mahila College, Amreli 365601, Gujarat, India

DOI:

https://doi.org/10.22159/ijap.2022v14i5.45517

Keywords:

Venlafaxine HCl, Oral organogel, Controlled release, One-factor response surface methodology

Abstract

Objective: The aim of this study was to develop the oral Venlafaxine HCl controlled-release organogel (organogel–CR) by using one-factor response surface methodology (RSM).

Methods: In this study, Drug-excipient compatibility was evaluated by FT-IR. A total of 14 experimental runs were carried out employing the detailed conditions designed by a single factor completely randomized design based on the response surface methodology was used to check the concentration effect of 12-Hydroxy stearic acid (12-HSA) at different cooling rates on drug release at 10 h (Q₁₀) and after 12 h (Q₁₂). Multiple linear regression analysis, analysis of variance (ANOVA) and graphical representation of the influence factor were performed by using design expert 12. The developed organogel was also evaluated for viscosity, strength, transition temperature, diffusivity and Scanning electron microscopy (SEM). Prepared organogel was filled in the capsule and investigated for weight variation, drug content, erosion of organogel and In vitro drug release study.

Results: FT-IR results showed that there was no chemical interaction between the drug and excipients. The SEM photograph indicates that the developed organogel was highly viscous with 3D network structure. The experimental confirmation tests showed a correlation between the predicted and experimental responses (R2 = 0.9937 and 0.9709). The results of ANOVA suggested that calculated F values of all dependent variables are greater than tabulated values. The optimal point obtained was located in the valid region and the optimum in vitro release of the predicted batch containing 7.9% concentration of 12-HSA with gradual cooling rate. To validate the evolved mathematical models, a checkpoint was selected and its desirability value was found to be 0.866.

Conclusion: Oral controlled release Venlafaxine HCl organogel fix the problem of repeated dosing and patient noncompliance.

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References

Andrews JM, Ninan PT, Nemeroff CB. Venlafaxine: a novel antidepressant that has a dual mechanism of action. Depression. 1996;4(2):48-56. doi: 10.1002/(SICI)1522-7162(1996)4:2<48:AID-DEPR2>3.0.CO;2-B, PMID 9160640.

Olver JS, Burrows GD, Norman TR. Third-generation antidepressants: do they offer advantages over the SSRIs? CNS Drugs. 2001;15(12):941-54. doi: 10.2165/00023210-200115120-00004, PMID 11735614.

Holliday SM, Benfield P. Venlafaxine. A review of its pharmacology and therapeutic potential in depression. Drugs. 1995;49(2):280-94. doi: 10.2165/00003495-199549020-00010, PMID 7729333.

Haskins JT, Moyer JA, Muth EA, Sigg E. Inhibition of noradrenergic neuronal activity by the novel bicyclic compounds, Wy-45030 and Wy-45881. Soc Neurosci 1984;10:262.

Troy SM, Parker VD, Fruncillo RJ, Chiang ST. The pharmacokinetics of venlafaxine when given in a twice-daily regimen. J Clin Pharmacol. 1995;35(4):404-9. doi: 10.1002/j.1552-4604.1995.tb04081.x, PMID 7650231.

Jyoti P. Development and optimization of extended-release venlafaxine HCl matrix tablet. Asian J Pharm Tech Innov. 2013;3(2):76-80.

Jain S, Datta M. Montmorillonite-alginate microspheres as a delivery vehicle for the extended oral release of venlafaxine hydrochloride. J Drug Deliv Sci Technol. 2016;33:149-56. doi: 10.1016/j.jddst.2016.04.002.

Dilip M, Kumbhar VD, Havaldar KKM, Remeth JD, Vishwajeet SG, Rahul B. Londhe. Formulation and evaluation of sustained release tablets of venlafaxine hydrochloride for the treatment of depressive disorders. Asian J Pharm Res. 2017;7(1):8-14.

Jose J, Gopalan K. Organogels: A versatile drug delivery tool in pharmaceuticals. Res J Pharm Technol. 2018;11(3):1242-6. doi: 10.5958/0974-360X.2018.00231.7.

Purohit B, Gupta N, Jain S. Formulation and evaluation of diclofenac sodium organogel. Res J Pharm Technol. 2013;6(4):375-8.

Nithya R, Kumari B. Development and characterization of reverse micelle based pluronic lecithin organogel containing imatinib mesylate. Res J Pharm Technol. 2021;14(3):1209-14. doi: 10.5958/0974-360X.2021.00215.8.

Abdelmonem R, Eltahan M, El-Nabarawi M. Development and evaluation of taste masked oro-disintegrating tablets of itopride hcl using different co-processed excipients: pharmacokinetics study on rabbits. Int J App Pharm. 2022;14(3):69-79. doi: 10.22159/ijap.2022v14i3.44398.

Carlson E, Chandler W, Galdo I, kudla T, Ta C. Automated integrated forced degradation and drug-excipient compatibility studies. JALA: Journal of the Association for Laboratory Automation. 2005;10(6):374-80. doi: 10.1016/ j.jala.2005.09.005.

Garg T, Bilandi A, Kapoor B. Oraganogel advanced and novel drug delivery system. Int Res J Pharm. 2011;2(12):15-21.

Fayez SM, Gad S. Formulation and evaluation of etodolac lecithin organogel transdermal delivery systems. Int J Pharm Pharm Sci. 2005;7:325-34.

Jayaprakash R, Hameed J, Anupriya A. An overview of transdermal delivery system. Asian J Pharm Clin Res. 2017;10(10):36-40. doi: 10.22159/ajpcr.2017.v10i10.19909.

Sharma G, Devi N, Thakur K, Jain A, Katare OP. Lanolin-based organogel of salicylic acid: evidences of better dermatokinetic profile in imiquimod-induced keratolytic therapy in BALB/c mice model. Drug Deliv Transl Res. 2018;8(2):398-413. doi: 10.1007/s13346-017-0364-9, PMID 28224375.

Vigato AA, Querobino SM, de Faria NC, de Freitas ACP, Leonardi GR, de Paula E. Synthesis and characterization of nanostructured lipid-poloxamer organogels for enhanced skin local anesthesia. Eur J Pharm Sci. 2019;128:270-8. doi: 10.1016/j.ejps.2018.12.009, PMID 30553060.

Vintiloiu A, Leroux JC. Organogels and their use in drug delivery-a review. J Control Release. 2008;125(3):179-92. doi: 10.1016/j.jconrel.2007.09.014, PMID 18082283.

Patil IS, Patil OA, Mandake GCR, Nitalikar MM. Development and evaluation of telmisartan pulsatile drug delivery by using response surface methodology. Asian Journal of Pharmaceutical Research 2018;8(4):205-14. doi: 10.5958/ 2231-5691.2018.00035.7.

Mahesh PG, Jeganath S. Formulation and evaluation of venlafaxine hydrochloride sustained release matrix tablet. Asian J Pharm Clin Res. 2018;11(16):170-4.

Upadhyay KK, Tiwari C, Khopade AJ, Bohidar HB, Jain SK. Sorbitan ester organogels for transdermal delivery of sumatriptan. Drug Dev Ind Pharm. 2007;33(6):617-25. doi: 10.1080/03639040701199266, PMID 17613026.

Aimetti AA, Machen AJ, Anseth KS. Poly(ethylene glycol) hydrogels formed by thiol-ene photopolymerization for enzyme-responsive protein delivery. Biomaterials. 2009;30(30):6048-54. doi: 10.1016/j.biomaterials.2009.07.043. PMID 19674784.

Swain S, Behera A, Dinda SC, Patra CN, Jammula S, Beg S. Formulation design, optimization and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharm Sci. 2014;76(4):354-63. PMID 25284934.

Duangjit S, Kraisit P. Optimization of orodispersible and conventional tablets using simplex lattice design: the relationship among excipients and banana extract. Carbohydr Polym. 2018;193:89-98. doi: 10.1016/j.carbpol.2018.03.087, PMID 29773401.

Kraisit P, Sarisuta N. Development of triamcinolone acetonide-loaded nanostructured lipid carriers (NLCs) for buccal drug delivery using the box-Behnken design. Molecules. 2018;23(4):E982. doi: 10.3390/molecules23040982, PMID 29690622.

Adan J, Singh R. Formulation and evaluation of Aloe vera topical gels. Int J Phys Sci. 2010;2:551-5.

Pathan IB, Shingare PR, Kurumkar P. Formulation design and optimization of novel mouth dissolving tablets for venlafaxine hydrochloride using the sublimation technique. J Pharm Res. 2013;6(6):593-98. doi: 10.1016/j.jopr.2013.04.054.

Sharma D, Kaur D, Verma S, Singh D, Singh M, Singh G. Fast dissolving oral films technology: a recent trend for an innovative oral drug delivery system. Int J Drug Deliv. 2015;7(2):60-75.

Kraisit P. Impact of hydroxypropyl methylcellulose (HPMC) type and concentration on the swelling and release properties of propranolol hydrochloride matrix tablets usning a simplex centroid design. Int J Appl Pharm. 2019;11:143-51. doi: 10.22159/ijap.2019v11i2.31127.

Duangjit S, Kraisit P. Optimization of orodispersible and conventional tablets using simplex lattice design: the relationship among excipients and banana extract. Carbohydr Polym. 2018;193:89-98. doi: 10.1016/j.carbpol.2018.03.087, PMID 29773401.

Sankalpa KB, Mathew SM. Response surface optimization of extraction parameters of green tea. Int J Agric Environ Biotechnol. 2017;10(2):209. doi: 10.5958/2230-732X.2017.00024.9.

Yu LX, Amidon G, Khan MA, Hoag SW, Polli J, Raju GK. Understanding pharmaceutical quality by design. AAPS J. 2014;16(4):771-83. doi: 10.1208/s12248-014-9598-3, PMID 24854893.

Collins LM, Dziak JJ, Li R. Design of experiments with multiple independent variables: a resource management perspective on complete and reduced factorial designs. Psychol Methods. 2009;14(3):202-24. doi: 10.1037/a0015826, PMID 19719358.