Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide

Abstract

The investigation deals with the affection of permeation of mupirocin from the Bactroban® Leciva ointment through full-thickness pig ear skin by the original Czech compound (S)-8-methyl-6,9-diazaspiro[4.5]decan-7,10-dione, known under the international non-proprietary name of “alaptide“, in micronized or nanonized form. It was found out that micronized alaptide significantly enhanced the permeation of mupirocin within 1 h after administration (approx. 5-fold). On the other hand, nanonized alaptide almost completely inhibited permeation of mupirocin from Bactroban® Leciva through the skin. Rapid primary screening showed that the two forms of alaptide influence differently the depth and the rate of permeation/penetration of mupirocin into/through the skin, i.e. affect curative effect of mupirocin on/in skin immediately after application of drug formulation.