FORMULATION AND EVALUATION OF ANTIFUNGAL PRONIOSOMAL GEL FOR ORAL CANDIDIASIS

Abstract

Fluconazole is a synthetic antifungal drug, belonging to triazole group and mostly used to treat oral candidiasis caused by the yeast Candida albicans. Fluconazole commercially available in tablets that offer poor bioavailability, due to hepatic first pass effect and gastric instability leads to frequent dosing. Buccal drug delivery can bypass such problems of tablet and leads to increase in bioavailability. Due to low molecular weight, fluconazole can suitably administered by buccal route, hence local and targeted action can achieve. The present study was conducted to develop proniosomal gel of fluconazole by coacervation phase separation method using Span 20, cholesterol, soya lecithin, ethanol and aqueous vehicle. Based on preliminary studies surfactant and aqueous vehicle was selected. The Box Behnken design was employed to optimized proniosomes by evaluating responses like entrapment efficiency, vesicle size and drug release. The optimized proniosomes were evaluated with entrapment efficiency (96.83%), vesicle size (2µm), in-vitro drug release 85.66 % (3 h) and ex vivo mucosal permeation (85.67 %) with flux (394.09 μg/cm2h). The optimized proniosomes were incorporated into 2% w/w Carbopol gel 934 (1:1) to obtain proniosomal gel. This optimized proniosomal gel was found with good viscosity, good spreadability and adhesiveness, also it shows maximum drug release and permeation as compared to plain gel of fluconazole. In microbiological studies, optimized formulation shows the maximum inhibitory effect as compared to plain gel of drug, which concluded that optimized proniosomal gel exerted local and targeted buccal delivery with good fungistatic effect than plain gel of fluconazole against Candida albicans. Keywords: proniosomal gel, oral candidiasis, fluconazole, mucoadhesion, Candida albicans.