Bioadhesive Garlic and Ketoconazole Vaginal Tablets for Treatment of Candidiasis

Abstract

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 3 2 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.

Antimicrobial Activity and Chemical Composition Screening of Anacyclus pyrethrum Root

“…The difference between our study and previous studies could depend on several reasons: (1) the microorganism strains used in these two studies may be different, (2) the location and collection season of A. pyrethrum may cause a change in active components, (3) the amount of extracts tested on microorganisms were different and (4) the type of extraction solvent may change the active compounds extracted from plant samples. According to Table 2, Palmitic acid (13.39%), Naphthalene, decahydro-1,1-dimethyl-(10.86%), 9,12-Octa decadienoic acid (Z,Z)-(10.10%), N-Isobutyl-tetradeca-2,4-dienamide (7.60%), 7-Tetradecenal, (Z)-(7.08%), Benzofuran-2-carboxaldehyde (5.50%) and.…”

“…1,2 Anacyclus pyrethrum (pellitory, Spanish chamomile or Mount Atlas daisy) root and leaf are important in traditional health and herbal medicine. In particular, A. pyrethrum root is known to have a good effect in traditional medical uses.…”

Antimicrobial Activity and Chemical Composition Screening of Epilobium montanum Root

“…But unfortunately microorganisms, including viruses, are still on the agenda of the scientist, because diseases caused by them are still threatening the public health especially in the developing countries, despite the remarkable progression in the medicine. [1][2][3] The growing number of new resistant pathogens direct the researches to discover new antimicrobial agents inevitably. Plants are accepted to be good candidates of being sources for new drug hits.…”

Solubility Enhancement of Poorly Water-Soluble Drug Ritonavir using Polyvinylpyrrolidone and Chitosan-based Platform Technique

“…It was then spectrophotometrically examined using a UV-vis spectrophotometer operating at 288 nm on the dissolved samples. [28][29][30]…”