Abstract

Skin penetration enhancers are molecules which reuersibly remove the barrier resistance of the stratum corneum. They allow drugs to penetrate more readily to the viable tissues and thus enter the systemic circulation. This paper presents a general theory for enhancer activity based on possible alterations at the molecular level of the stratum corneum. Within the intercellular route, accelerants may interact at the polar head groups of the lipids, within aqueous regions between lipid head groups, and between the hydrophobic tails of the bilayer. Within the corneocyte the keratin fibrils and their associated water provide the target. High concentrations of solvents may also alter partitioning phenomena. The theory has been applied specifically to water, Azone, dimethylsulfoxide, dimethylformamide, 2-pyrrolidone, N-methyl-2-pyrrolidone, oleic acid, decylmethylsulfoxide, sodium lauryl sulfate and propylene glycol. The main techniques which supplied experimental support for the theory were permeation studies through human skin, the vasoconstrictor assay and differential scanning calorimetry; the results from DSC are mainly considered here.

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