Boyko Y. Influence of cholesterol and its esters on the transdermal penetration of 1,4-benzdiazepine derivatives

Biological activity of organic compounds as strengtheners of skin permeability. A purpose is a search of new effective strengtheners of skin permeability among the derivatives of cholesterol and esteriv of polyols. Research methods - chemical, pharmacological, biochemical, statistical. Cholesterol and its esters, liquid crystal systems cholesterol esters, unsaturated acids and esters of polyatomic alcohols were studied as chemical permeability enhancers. The influences of these compounds on the physico-chemical properties of lipid membranes (including the stratum corneum liposomes) were studied by methods of membrane probes and infrared spectroscopy. The influence of all enhancers on the permeability of 14C-phenazepam through the stratum corneum of the epidermis was studied in vitro. We have found that all investigated substances can be used as enhancers of transdermal permeability (concentration - 10% in the composition of transdermal systems). There are a number of clinical conditions requiring urgent administration methods, which have been observed in the immediate therapeutic effect. It is recommended to use a transdermal therapeutic system designed in medical practice on the basis of cholesterol ester mixtures as they provide dosage forms delivering the drug quickly and efficiently. Sphere of use - bioorganic chemistry, medicine.