Formulation and Evaluation of Antifungal Drug Containing Mucoadhesive Tablet for Vaginal Candidiasis

Abstract

Objectives: Female population frequently seeks medical consultation for the vaginal candidiasis. Voriconazole (VOR) is a BCS class II antifungal drug with low aqueous solubility and hence inclusion complex was formulated using Hydroxypropyl--cyclodextrin (HPCD). The complex was incorporated into mucoadhesive vaginal tablet using Chitosan and Hydroxypropyl Methyl Cellulose (HPMC K100).Materials and Methods: A 3^2 full factorial design was employed for sustained release tablet using Design expert software.Results: Scanning Electron Microscopy (SEM) results indicated the complex formation between the drug and HPCD. The batches showed 39.681.2 to 72.311.4% of drug release for 4 hr while for 8 hr it was from 77.231.5 to 99.821.1%. Therefore, the sustained release of drug was achieved for 8 hr. The tablet batches had swelling % from 228.5112 to 323.118% and mucoadhesive strength from 1131.0249 to 2302.1255 dyne/cm^2. In the in vitro antifungal activity study, a higher zone of inhibition was observed for the inclusion complex-based tablet (340.3 mm) as compared to plain drug tablet (250.4 mm).Conclusion: Therefore, the inclusion complex-based vaginal tablet could be formulated successfully by employing 3^2 full factorial design for increased residence of drug at the vaginal site of infection and for improved therapeutic efficacy.

Keywords: Voriconazole; Factorial design; Inclusion complex; Vaginal Candidiasis; Sustained release; In vitro antifungal activity; In vitro release