Effects of Absorption Enhancers and Lipid Composition on Drug Permeability through the Model Membrane Using Stratum Corneum Lipids

抄録

We have developed a model membrane system for estimating drug permeability of skin by fixing liposomes composed of stratum corneum (SC) lipids (ceramides, palmitic acid, cholesterol, and cholesterol-3-sulfate) onto a supporting filer, Biodyne B (Chem. Pharm. Bull., 41, 575 (1993)). In both the model membrane and guinea pig skin experiments, the addition of absorption enhancers (Azone, decylmethylsulfoxide, oleic acid, and capric acid)caused an increase in cyclobarbital (a relatively hydrophilic drug) permeation, but had littel effect on ibuprofen (a hydrophobic drug) permeation. Thus, the model membrane and guinea pig skin behave similarly in terms of permeability, suggesting that the main target of the enhancers is the SC intercellular lipid lamellae. The influence of SC lipid composition on permeability was also investigated. A lipid composition similar to that of skin SC showed the lowest permeability for the hydrophilic drug. Our model membrane system was found to be widely applicable for drug permeation studies.