Formulation and In Vitro Characterization of Ketoconazole Span 80 Based Transfersomes Gel, Its Comparison with Liposomal Gel and Evaluation of Antimicrobial Activity

摘要

The objective of this study was to formulate, optimize and evaluate ketoconazole transfersomes gel. Sixteen formulations of ketoconazole loaded transfersomes were prepared by conventional thin layer evaporation technique using design expert software. The effect of independent process variables like concentration of soya lecithin and surfactant on dependent variable such as entrapment efficiency and vesicle size of Ketoconazole transfersomes using face centered central composite designs was determined. The transfersomes formulation K7 (span 80 based) was found to have highest entrapment efficiency (86.4 ±0.61%) followed by K2 (tween 80 based) (73.36 ± 0.58%) followed by K14 (sodium deoxycholate based) (59.75 ±0.36%). It was observed that entrapment efficiency of K7-span80 transfersomes formulation was significantly higher than that of liposomal suspension K21 (30.54 ±0.45%). Span 80 was selected as the suitable carrier with highest entrapment efficiency and vesicle size of 2.56 ±0.21 μm. The optimized K7 suspension was further incorporated into gel (KS19) and showed maximum drug content (99.78±0.03%), maximum drug release (86.92 ±0.43%). Release of Ketoconazole from final gel followed Korsmeyer peppas release model (r~2 = 0.99). The formulation showed proper semisolid consistency and good stability at the end of 3 month at 2-8 °C compared to liposomal gel and plain gel (KG 26). Antifungal activity showed that the developed KS19 was more active against yeast Candida albicans as compared to liposomal gel and plain gel. These results suggest that the developed Ketoconazole loaded transfersomes gel can be a potentially useful novel formulation as compared to liposomes.