EUDRAGIT S-100 MICROSPONGES BASED GEL OF BUTENAFINE HYDROCHLORIDE FOR CANDIDIASIS: DESIGN, OPTIMIZATION, IN VITRO AND IN VIVO INVESTIGATION

Objective:This research focused on formulating a controlled-release microsponge gel incorporating Butenafine hydrochloride (BFH), designed to enhance drug retention time and reduce the risk of skin irritation. Methods:BFH-loaded microsponges were prepared using the quasi-emulsion solvent diffusion technique. Optimization of formulation parameters, including eudragit S-100 and dichloromethane, was performed using a 32-factorial design. The microsponges were evaluated for production yield, entrapment efficiency, and cumulative drug release using FTIR, XRD, DSC, and SEM techniques. The optimized microsponge formulation was incorporated into a Carbopol 934 gel. The resulting microsponge gel was assessed for extrudability, spreadability, drug content, in-vitro drug release, rheological properties, and in-vitro antifungal activity against Candida albicans. Results:The optimized microsponge formulation exhibited a particle size of 48.92 ± 2.49 µm, an entrapment efficiency of 89.42 ± 1.55%, and a cumulative drug release of 81.67 ± 2.41%. The microsponge gel demonstrated a controlled drug release and was non-irritant to rat skin. The controlled release of butenafine hydrochloride from the microsponge gel resulted in prolonged drug retention with reduced permeation activity. Conclusion:The study revealed that the butenafine hydrochloride microsponge gel offers enhanced topical retention and prolonged drug release. Additionally, it showed superior antifungal activity compared to marketed preparations while significantly reducing skin irritation.