Formulation and evaluation of mucoadhesive fluconazole vaginal tablets

Abstract

Objective: Fluconazole is a triazole antifungal agent, and is used to treat fungal infections but because of frequent dosing and undesirable side effects it affects patient compliance. There came the need for a delivery system that can skip first pass metabolism and adhere long enough to treat the infection effectively, that was the aim for this study. Mucoadhesive drug delivery system adheres to mucous membrane and provide prolonged and sustained drug release. Method: Five formulations were formed by granulation method. The granules were then compressed and tablets were formed each of 250mg. Different evaluation parameters were determined like hardness, friability, weight variation, content uniformity, mucoadhesive strength, swelling index, dissolution and compatibility analysis. Results: The hardness (7.2-8.9kg), friability (0.02-0.05%), weight variation (0.1-0.4%), content uniformity (96.9-103%), were all in the pharmacopeial range. Dissolution was determined using rotating paddle apparatus with a phosphate buffer of 6.8 pH. Release kinetics showed that F1, F2, F3 showed Fickian release while F4 showed both Fickian and non Fickian release and F5 showed non Fickian release. Mucoadhesive strength was found to be the highest (46g) in formulation F5. The highest swelling index (70.34%) was shown by formulation F3 at 12h. Differential scanning calorimeter and Fourier transform infrared spectroscopy showed that there is no interaction between excipients. Conclusion: Hence, results showed that fluconazole vaginal tablets can be formed by using these ingredients and formulation F5 was the most optimum formulation.