Transdermal penetration enhancers

The paper presents the first systemic classification and analysis of transd ermal penetration enhancer structures from the point of view of medicinal c hemistry. The mechanism of effect of these compounds is not based on a rece ptor interaction, nevertheless we have found some structural regularities o f the enhancing effect. Molecules of the most effective enhancers nearly al ways contain a fragment of the natural moisturising factors present in huma n skin at normal physiological conditions. The simplest structural fragment of efficient enhancers is X-CO-N = where X, is -CH2-, -NH2, -NH-, and it s hould contain a long alkyl or alkenyl (C-8-C-20) chain as well, including p ossible isosteric modifications. The omega-amins acid derivatives as the su bstances complying fully with these criteria, have been intensely studied.