Permeation of Indomethacin through Skin Using Nanonized Alaptide

Abstract

Alaptide, (S)-8-methyl-6,9-diazaspiro[4.5]decan-7,10-dione, is an original Czech compound; in this paper it is used as an excipient. The investigation deals with the affection of the permeation of indomethacin through full-thickness pig ear skin using a Franz diffusion cell from the donor vehicle of propylene glycol/water (1:1) using nanonized alaptide as a potential transdermal permeation enhancer. Alaptide was applied in ratio 1:10 (w/w) related to the amount of indomethacin. Nanonized alaptide showed an excellent rapid onset of enhancement effect, already at the 30th minute after application, when the permeated amount of indomethacin was 5-fold more than in the formulation without alaptide. The enhancement ratio of nanonized alaptide was 5.6, which indicates that alaptide modifies skin structure, which results in significantly enhanced permeation at long-term application.