EFFECT OF PENETRATION ENHANCERS ON THE PERMEABILITY OF KETOCONAZOLE GELS THROUGH RABBIT SKIN

Document Type : Original Article

Authors

Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt

Abstract

The influence of several penetration enhancers on the percutaneous penetration of ketoconazole (KC) from hydroxypropylmethyl cellulose (HPMC), sodium carboxymethyl cellulose (NaCMC) and carbopol 934 gel formulations was investigated. Skin permeation studies were performed using Franztype diffusion cells and full-thickness abdominal rabbit skin. Various types of compounds such as oleic acid (OA), menthol (M) and isopropyl myristate (IPM) in various concentrations were employed as penetration enhancers. The steady-state flux, permeability coefficients, and enhancement ratios ER flux of KC for each formulation were calculated. The results showed that the skin permeability of KC from gels tested was significantly increased (P< 0.05) by 10% w/w OA, 5% w/w M and 5% w/w IPM. ER flux of KC gels containing 10% OA were 19.5, 16.4 & 11.9 for NaCMC, HPMC & carbopol gel respectively. ERflux of 5% w/w M were 13.5, 13.3 & 10.9 for HPMC, NaCMC & carbopol gel respectively. About 11 fold increase in the ERflux at 5% w/w IPM for all gels. Kinetic analysis of the data indicated that the permeation of (KC) from different gel formulations obeyed Higuchi-diffusion model. In conclusion, OA, M & IPM could be considered as penetration enhancers for KC topical formulations.

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