Alaptide as Transdermal Permeation Modifier

Abstract

Based on the fact that alaptide is able to influence the creation and function of keratinocytes, it was supposed that alaptide could be used as a transdermal permeation modifier. Various APIs (bases, acids, salts, neutral molecules, small molecules, steroid-like molecules) were tested on their transdermal permeation in the mixture with micronized and/or nanonized alaptide as a transdermal permeation modifier. Also the influence of the type of formulation (ointment, cream, gel) on the effect of alaptide on skin was investigated intensively. It was observed that under specific conditions alaptide is able to suppress permeation/absorption of compounds through the skin, which can limit the site of action of potentially hazardous/toxic drugs to skin surface. The skin curative activity of alaptide can be helpful in reduction of possible skin irritant/injurious effects of permeating compounds. In transdermal application alaptide causes an increase or a decrease, in dependence on the used concentration, physical state and supporting medium (pharmaceutical formulation), in permeation/absorption of drugs into the skin and/or through the skin. The concentration of the used drug was increased at the place of administration, and/or the systemic concentration was increased, or it was ensured that drugs acted only on the skin surface/in the skin surface layer and did not penetrate into the deeper skin layers or did not have any systemic effect. Although alaptide was found in the 1980s of the twentieth century, even now it has great potential either as an active pharmaceutical ingredient or a permeation modifier.

Dr. Evžen Kasafírek, the “parent” of the alaptide molecule who tragically left us, was an excellent medicinal chemist who was undervalued in his lifetime. He left us many results of his creative work. He educated experts who hold top positions in the world’s largest pharmaceutical companies. We dedicate this article to his memory.