Formulation Development and Evaluation of Mucoadhesive Vaginal Film of Fluconazole

Abstract

The aim of the present investigation was formulation, development and evaluation of mucoadhesive vaginal film of fluconazole which provides prolonged contact of dosage form with vaginal mucosa and controlled release of drug leading to better treatment of vaginal candidiasis. Fluconazole is triazole derivative antimycotic drug applied locally for the treatment of vaginal candidiasis. Mucoadhesive antifungal vaginal film was formulated using Chitosan and Pectin as a film forming polymer and glycerol as a plasticizer. Drug excipients compatibility study was carried out using Differential Scanning Colorimetry and Fourier Transformed Infrared Spectroscopy. The mucoadhesive vaginal films were evaluated for Thickness, % Elongation, Tensile strength, Drug diffusion, Moisture content, Swelling study, Drug content and folding endurance. Amongst Various permeation enhancers used, DMSO was selected. To evaluate the role of concentration of DMSO and concentration of Glycerol in optimization of vaginal film, 32 full factorial design was selected. Optimized batch F10 showed 8.7 N/mm2 Tensile strength, 10 % Elongation, 2.5% Moisture content, 2.2 Swelling study and 79 % drug diffusion in 24 hour. The optimized batch was further evaluated by Scanning electron microscopy indicating uniform surface of the film. Invitro antifungal activity of optimized batch showed inhibitory effect against C. albicans and did not adversely affect the growth of Lactobacillus, a normal component of vaginal flora. The optimized film formulation was compared with the marketed fluconazole gel (Flucos) which indicates controlled release of drug than gel. Initially sustained release of drug was observed in ex vivo diffusion study using rat vaginal skin as compared to in vitro diffusion of optimized film. In vivo irritation study was performed with optimized batch F10 and marketed Flucos gel. It was concluded that there was no vaginal irritation in either of the formulation. Stability study was carried out of optimized batch F10 for 1 month at 40°C/75% RH and 25°C/60% RH. It was conducted that mucoadhesive vaginal film provided controlled release of fluconazole in effective treatment of vaginal candidiasis.