A 32 FULL FACTORIAL DESIGN FOR TOPICAL CONTROLLED RELEASETAZAROTENE MICROSPONGE USING HPMC GEL
Objective: The aim of present work was to the development of control release 0.1% tazarotene microsponge and incorporated into a HPMC K-100M gel.
Methods: Drug compatibility with polymer was evaluated by FT-IR spectrum. Tazarotene microsponge was prepared by quasi-emulsion solvent diffusion method. On the basis of preliminary results, 32 full factorial design was employed to study the effect of Eudragit RS-100 conc. (X1) and PVA conc. (X2) on as particle size (Y1), % drug entrapment (Y2) and time required to 80% drug release (Y3). Multiple linear regression analysis, ANOVA and graphical representation of the influence factor by 3D plots were performed by using Sigma plot 11.0. In this study, the following constraints were arbitrarily used for the selection of an optimized batch: particle size<200 µm, drug entrapment>70 %, and time required to 80% drug release>360 min. The optimized formulation was subjected to SEM study. Tazarotene microsponge incorporates in 3% HPMC K-100M gel evaluated for viscosity, pH, drug content, spreadability, In vitro diffusion study, release kinetic study and photostability study.
Results: The FT-IR result showed that there was no chemical interaction and SEM photograph indicates that microsponges are spherical and pores. From the results of multiple regression analysis, it was found that all factors had a statistically significant influence on all dependent variables.
Conclusion: The optimized formulation of gel release kinetics having good linearity (R2= 0.987) of zero-order kinetic and it was found to be stable in the stability evaluation.
2. Mehta M, Panchal A, Shah VH, Upadhyay U. Formulation and in vitro evaluation of controlled release microsponge gel for topical delivery of clotrimazole. Int J Adv Pharm 2012;2:93-101.
3. Weinstein GD. Tazarotene gel: efficacy and safety in plaque psoriasis. J Am Acad Dermatol 1997;37:33–8.
4. Weinstein GD, Krueger GG, Lowe NJ. Tazarotene gel, a new retinoid, for topical therapy of psoriasis: vehicle-controlled study of safety, efficacy, and duration of therapeutic effect. J Am Acad Dermatol 1997;37:85–92.
5. Shalita AR, Chalker DK, Griffith RF. Tazarotene gel is safe and effective in the treatment of acne vulgaris: a multi-center, double-blind, vehicle-controlled study. Cutis 1999;63:349–54.
6. Oza N, Trivedi R, Swati S. Systemic enhancement of nebivolol by using nanosuspension in-situ nasal spray. Inventi Rapid: NDDS; 2019. p. 1-8.
7. Carlson E, Chandler W, Galdo I, kudla T. Automated integrated forced degradation and drug-excipients compatibility studies. J Assoc Lab Autom 2005;10:374-80.
8. Burcu D, Kandemir C. Preparation and evaluation of modified release ibuprofen microspheres with acrylic polymers (eudragit®) by quasiemulsion solvent diffusion method: effect of variable. Acta Poloniae Pharm Drug Res 2006;63:521-34.
9. R Ravi, SK Senthil Kumar, S Parthiban. Formulation and evaluation of the microsponge gel for an anti-acne agent for the treatment of acne. Int J Pharm Sci Res 2013;3:32-8.
10. Yadav V, Jadhav P, Dombe S, Bodhe A, Salunkhe P. Formulation and evaluation of microsponge gel for topical delivery of antifungal drug. Int J Appl Pharm 2017;9:30-7.
11. Durgapal S, Mukhopadhyay S, Goswami L. Preparation, characterization and evaluation of floating microparticles of ciprofloxacin. Int J Appl Pharm 2017;9:1-8.
12. Jadhav N, Patel V, Mungekar S, Bhamare G, Karpe M, Kadams V. Microsponge delivery system: an updated review, current status and future prospects. J Sci Ind Res 2013;2:1097-110.
13. P Yadav, S Nanda. Development and evaluation of some microsponge loaded medicated topical formulations of acyclovir. Int J Pharm Sci Res 2014;5:1395-410.
14. Kumar RG, Sanghvi I. Optimization techniques: an overview for formulation development. Asian J Pharm Res 2015;5:217-21.
15. Ugurlu T, Rayaman E, Karacicek U. Optimization and evaluation of clarithromycin floating tablets using experimental mixture design. Acta Pol Pharm 2014;71:311-21.
16. Hamid H, Archana D, Divya J, Abhishek B. Formulation and evaluation of gel-loaded microsponges of diclofenac sodium for topical delivery. Pharm Innov J 2014;3:58-63.
17. Klich CM, Jels, Jellies. In: Swarbrick J, Boylan JC. Encyclopedia of pharmaceutical technology. New York, NY: Marcel Dekker Inc; 1992;6:415-39.
18. Atmaram PP, Aditya P, Ashwin BK, Bothiraja C, Ashwin JM. Formulation and evaluation of optimized oxybenzone microsponge gel for topical delivery. J Drug Del 2015. http://dx.doi.org/10.1155/2015/261068
19. Osmani RA, Aloorkar NH, Kulkarni AS. Novel cream containing microsponges of anti-acne agent: Formulation development and evaluation. Curr Drug Delivery 2015;12:504-16.
20. NS Abdelmalak, SF El-Menshawe. A new topical fluconazole microsponge loaded hydrogel: preparation and characterization. Int J Pharm Pharm Sci 2012;4:460–9.
21. Kaundal A, Bhatia R, Sharma A, Sukrial P. A review on microsponges drug delivery system. Int J Adv Pharm 2014;4:177-81.
22. Benita S, Donbrow M. Dissolution rate control of the release kinetics of water-soluble compounds from ethyl cellulose film-type microcapsule. Int J Pharm 1982;12:251-64.
23. Dash S, Murthy P, Nath L. Kinetic modeling on drug release from controlled drug delivery systems. Pharm Drug Res 2010;67:217-23.
24. Stability testing of new drug substances and products [Q1A (R2)]. The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH); 1996.
25. Vogel AI. Vogel's textbook of quantitative chemical analysis. 5th ed. Jeffrey GH, Bassett J, Mendham J, Denney R. editors; 1989. p. 220-5.
26. Bolton S, Bon C. Pharmaceutical statistics: practical and clinical applications. 5th ed. Informa Healthcare; 2005. p. 472-93.
27. Lewis GA, Mathieu D, Phan-Tan-Luu R. Pharmaceutical experimental design. New York: Marcel Dekker; 1999. p. 191-8.
28. Anthony NA. Pharmaceutical experimental design and interpretation. 2nd ed. Taylor and Francis Group; 2006.
29. Khanam N, Alam MI, MD Yusuf Ali, QMAI Siddiqui, A Ur Rahman. A review on the optimization of drug delivery system with experimental designs. Int J Appl Pharm 2018;10:7-12.
30. Madgulkar AR. Formulation and optimization of sustained-release tablets of venlafaxine resinates using response surface methodology. Indian J Pharm Sci 2009;71:387-94.
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