ESTERS OF OMEGA-AMINO ACIDS AS FLEXIBLE PENETRATION ENHANCERS

Series of esters of 6-aminohexanoic acid, 7-aminoheptanoic acid, and 8 -aminooctanoic acid were synthesized as candidates for novel skin pene tration enhancers. The permeation of theophylline expressed in the for m of the enhancement factor (EF) was studied with human cadaver skin b y a diffusion cell technique in the presence of the esters 1-17 in the water vehicle. The permeation in the presence of the 6-aminohexanoate s 1-5 was also studied in the olive oil vehicle. Of the compounds test ed, the most satisfactory enhancement in the water vehicle and oil veh icle were observed with octyl 6-aminohexanoate (EF = 45.5) and decyl 6 -aminohexanoate (EF = 19.5), respectively.