The FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE MICROSPONGE GEL

  • Tavva Vedavathi Dr

Abstract

The microsponge delivery system (MDS) which consists of microporous beads is the best technology for the controlled release of topical agents. Terbinafine hydrochloride is an antifungal agent used to treat nail antifungal infections (onychomycosis), but tends to accumulate in skin and nails when applied topically and shows some side effects like rash, irritation etc. 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. 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. A selected THCl 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, one (i.e. THMG II) showed better results like pH 6.2, viscosity 3960, spreadability 18.1g cm/s, drug content of 87.6% and drug release showed fickian release pattern. The antifungal studies showed the 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. 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.


 


 


 

Keywords: Antifungal, Gel, Microsponges, Terbinafine hydrochloride.

References

1. Aritomi H, Yamasaki Y, Yamada K, Honda H and Koshi M. Development of sustained release formulation of chlorpheniramine maleate using powder coated microsponges prepared by dry impact blending method. Journal of Pharmaceutical Sciences and Technology. 1996; 56(1): 49-56.
2. Jain NK. Advances in controlled and novel drug delivery. New Delhi: CBS Publishers and Distributors; 2003: 89-91.
3. Kydonius AF, controlled release technologies: Methods, Theory and Application, Boca Raton: CRC; 1980: 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: 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. Tropical Journal of Pharmaceutical Research. 2010; 9 (1): 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. International journal of pharmaceutics 2006; 308:124-32.
8. Kim W, Hwang S, Park J, Park H. Preparation and characterization of drug loaded polymetha-crylate 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 microparticulate 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 Control 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 Nov.
18. Novartis. Lamisil (terbinafine) oral granules prescribing information. East Hanover, NJ; 2007 Sept.
19. D’souza JI, Jagdish K, Saboji SG, Killedar HN. More “Design and Evaluation of Benzoyl Peroxide Microsponges to Enhance Therapeutic Efficacy in Acne Treatment”, Accepted for presentation in 20th fapa congress1, Bangkok , Thailand , Nov30-Dec 3 (2004).
20. Comoglu T, Gonul N, Baykara T. Preparation and In vitro evaluation of modified release ketoprofen microsponges. II Farmaco. 2003;58:0 101-6.

21. Orlu M, Cevher E, Araman A. Design and evaluation of colon-specific drug delivery system containing flurbiprofen microsponges, Inter J Pharmaceutics.2006; 318: 103-117.
22. Martin A, Swarbrick J, Cammarata AX, In: Physical Pharmacy- Physical Chemical Principles in Pharmaceutical Sciences. 3rd Ed, 1991 pp.527.
23. D’souza, JI , More, HN. Res J.Pharm Tech.2008; 1(4): 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 and Tissue Res. 2011; 11(1): 2691-6.
25. Loganathan V, Manimaran S, Sulaiman A, Reddy MVS, Senthil BK, Rajaseskar A. Indian J Pharm Sci.2001;63(3): 200-4.
26. Rao NGR, Rao KP, Muthalik S. Asian J Pharmaceutics.2009; 3: 125-34.
27. Kedor Hackmann ERM, Santoro, MIRM, Singh, AK, Peraro AC. Brazilian J. Pharm. Sci.2006; 42(1): 91-98.
28. Doijad, RC, Manvi, FV, Rao, SNM. and Alase, P.Indian J. PharmSci. 2006; 68(6): 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 Control 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; 57:274–77.
32. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of the 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, pp 100-107 (1996).
36. Satturwar PM, Fulzele SV, Nande VS, Khandare, JN. Indian J Pharm Sci.2002; 64(2) 155-8.
37. Harrison EF, Hamlow EE, Tavormina PA, Zygmunt WA. Appl Microbiol.1970;19 (5):746-50.
38. 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(4): 527–34.
Statistics
31 Views | Downloads
How to Cite
Vedavathi, T. (2019). The FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE MICROSPONGE GEL. International Journal of Applied Pharmaceutics, 11(6). Retrieved from https://innovareacademics.in/journals/index.php/ijap/article/view/32502
Section
Original Article(s)