FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE MICROSPONGE GEL
Objective: The purpose of the present research work was to formulate and evaluate Terbinafine hydrochloride microsponges using quasi emulsion solvent diffusion technique and microsponge gel by using carbopol for controlled release of the drug and consequently avoiding its side effects.
Methods: Microsponges containing Terbinafine hydrochloride were obtained successfully with six different drugs: polymer ratios. The formulations were studied for particle size, physical characterization, and in vitro release.
Results: A selected THCI microsponge (MS IV) due to its better results when compared to other microsponge formulations was incorporated in different concentrations of carbopol and formulated as gels and evaluated for its pH, viscosity, spreadability, drug content, in vitro release, antifungal activity and in vivo studies. Among the four microsponge gel formulations, THMG II showed better results like pH 6.2, viscosity 3960 cps, spreadability 18.1 g cm/s, drug content of 87.6% and drug release showed fickian release pattern. The antifungal studies showed a zone of inhibition with 15.8 mm when compared to the pure drug, 19.2 mm, marketed formulation 16.0 mm and also showed better antifungal activity on fungal induced guinea pig skin when compared with control.
Conclusion: In this study, we found that the controlled release of terbinafine hydrochloride from the microsponge gel reduced side effects and remarkably decreased gel application for fungal treatment.
2. Jain NK. Advances in controlled and novel drug delivery. New Delhi: CBS Publishers and Distibuters; 2003. p. 89-91.
3. Kydonius AF. Controlled release technologies: methods, theory and application, boca raton. CRC; 1980. p. 21-49.
4. Nacht S, Katz M. The microsponge: a programmable delivery system. In: Osborne, DW, Aman AH. Topical drug delivery formulations. New York: Marcel Dekker; 1990. p. 299-325.
5. Embil K, Ntcht S. The microsponge delivery system (MDS): a topical delivery system with reduced irritancy incorporating multiple triggering mechanisms for release of actives. J Microencapsul 1994;13:575-88.
6. Jain V, Singh R. Dicyclomine loaded Eudragit-based microsponge with potential for colonic delivery: preparation and characterization. Trop J Pharm Res 2010;9:67-72.
7. Jelvehgari M, Siahi Shadbad M, Azarmi S, Martin GP, Nokhodchi A. The microsponge delivery system of benzoyl peroxide: preparation, characterization and release studies. Int J Pharm 2006;308:124-32.
8. Kim W, Hwang S, Park J, Park H. Preparation and characterization of drug-loaded polymethacrylate microspheres by an emulsion solvent evaporation method. J Microencapsul 2002;6:811-22.
9. Kawashima Y, Niwa T, Hand T, Takeuchi H, Iwamoto T. Control of prolonged drug release and compression properties of ibuprofen microspheres with acrylic polymer by changing their intra-particle porosity. Chem Pharm Bull 1992;40:196-201.
10. Dashora K, Saraf S. Effect of processing variable in micro particulate system of nimesulide. Chinese J Pharm 2006;58:67-74.
11. Ameen M. Epidemiology of superficial fungal infections. Clin Dermatol 2010;28:197–201.
12. Hay R. Superficial fungal infections. Medicine 2009;37:610–2.
13. Ramos-e-Silva M, Lima CMO, Schechtman RC, Trope BM, Carneiro S. Superficial mycoses in immune depressed patients (AIDS). Clin Dermatol 2010;28:217–25.
14. Alberti I, Kalia YN, Naik A, Bonny JD, Guy RH. In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum. J Controlled Release 2001;71: 319–27.
15. Balfour JA, Faulds D. Terbinafine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in superficial mycoses. Drugs 1992;43:259–84.
16. Kazakov PV, Golosov SN. A simple method for obtaining terbi?nafine hydrochloride. Pharm Chem J 2004;38:34–6.
17. Novartis. Lamisil (terbinafine hydrochloride) tablets prescribing information. East Hanover. NJ; 2005.
18. Novartis. Lamisil (terbinafine) oral granules prescribing information. East Hanover. NJ; 2007.
19. 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.
20. Thireesha B, Prasad AR, Peter PLH. Formulation and evaluation of lornoxicam microsponges using eudragit rs 100 and eudragit rspo. Asian J Pharm Clin Res 2018;11:217-21.
21. Yadav V, Jadhav P, Dombe S, Bodhe A, Alunkhe P. Formulation and evaluation of microsponge gel for topical delivery of antifungal drug. Int J Appl Pharm 2007;9:30-7.
22. Martin A, Swarbrick J, Cammarata AX. In: Physical pharmacy-physical chemical principles in pharmaceutical sciences. 3rd Ed. Philadelphia: Willey; 1991. p. 527.
23. Dsouza JI, More HN. Topical anti-inflammatory gels of fluocinolone acetonide entrapped in eudragit based microsponge delivery system. Res J Pharm Tech 2008;1:502-6.
24. Saboji JK, Manvi FV, Gadad AP, Patel BD. Formulation and evaluation of ketocnazole microsponge gel by quasi emulsion solvent diffusion. J Cell Tissue Res 2011;11:2691-6.
25. Loganathan V, Manimaran S, Sulaiman A, Reddy MVS, Senthil BK, Rajaseskar A. Synthesis and anti-cancer activity of some L -cystine derivatives. Indian J Pharm Sci 2001;63:200-4.
26. Rao NGR, Rao KP, Muthalik S. Development and evaluation of carbamazepine fast dissolving tablets prepared with a complex by direct compression technique. Asian J Pharma 2009;3:125-34.
27. Kedor Hackmann ERM, Santoro, MIRM, Singh AK, Peraro AC. First-derivative ultraviolet spectrophotometric and high-performance liquid chromatographic determination of ketoconazole in pharmaceutical emulsions. Brazilian J Pharm Sci 2006;42:91-8.
28. Doijad RC, Manvi FV, Rao SNM, Alase P. Sustained ophthalmic delivery of gatifloxacin from In situ gelling system. Indian J Pharm Sci 2006;68:814-8.
29. Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123–33.
30. Husson I, Leclerc B, Spenlehauer G, Veillard M, Couarraze G. Modeling of drug release from pellets coated with an insoluble polymeric membrane. J Controlled Release 1991;17:163–73.
31. Schwartz JB, Simonell AP, Higuchi WI. Drug release from wax matrices: analysis of data with first-order kinetics and with the diffusion-controlled model. J Pharm Sci 1968;57:274–7.
32. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145–9.
33. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25–35.
34. Peppas NA. Analysis of fickian and non-fickian drug release from polymers. Pharm Acta Helv 1985;60:110–1.
35. Indian Pharmacopoeia. Govt. of India. Ministry of health and family welfare. Vol. 2. Delhi Pub Microbiol Assays; 1996. p. 100-7.
36. Satturwar PM, Fulzele SV, Nande VS, Khandare JN. Indian J Pharm Sci 2002;64:155-8.
37. Van Cutsem J, Van Gerven F, Van de Ven MA, Borgers M, Janssen PA. Itraconazole, a new triazole that is orally active in aspergillosis. Antimicrob Agents Chemother 1984;26:527–34.
38. El-Bagory IM, Hosny EA, Al-Suwayeh SA, Mahrous GM, Al-Jenoobi FI. Effects of sphere size, polymer to drug ratio and plasticizer concentration on the release of theophyline from ethylcellulose microspheres. Saudi Pharm J 2007;15:213–7.
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