Objective: The study represents design and development of a combination type of bioadhesive vaginal tablets of garlic and ketoconazole by direct compression for enhanced antifungal effect. Material and methods: In these, work ketoconazole tablets, garlic tablets, and garlic and ketoconazole combination tablets were prepared using 32 factorial design. HPMC K15M, chitosan, and microcrystalline cellulose were employed as bioadhesive polymers whereas, sodium bicarbonate and citric acid were incorporated to exert effervescence. Tablets were evaluated for swelling, bioadhesion and in-vitro drug release as dependent variables. The comparative in-vitro antifungal effects of optimized formulations were made with commercial tablets. Results: All tablet formulations exhibited sustained effect with moderate bio-adhesion characteristics. A tablet containing garlic: ketoconazole at 2:1.5 showed significant (p<0.05) in-vitro antifungal activity compared to reference tablet. Ex-vivo mucoadhesion times of formulations were ranged from 8 – 15 h. Enhanced antifungal activity is the result of the synergistic effect exerted by garlic with ketoconazole, as both are highly stable and soluble at pH 5. The synergistic effect produced by garlic with ketoconazole was proved by molecular docking studies, used to determine virtual interactions between them. Conclusion: The resulting outcome indicates that combination of the synthetic drug with natural actives could enhance the antifungal activity with a simultaneous reduction in drug dosage and side or toxic effects providing a potential tablet formulation to treat vaginal candidiasis.
Key words: Ketoconazole, Garlic, Bioadhesion, Vaginal candidiasis, Molecular docking.
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