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

Josef Jampilek,Radka Opatrilova

doi:10.5599/admet.2.1.26

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.

Highlights

Development in the field of pharmaceutical dosage forms results in the discovery of additional highly sophisticated drug delivery systems that allow for the maintaining of constant levels of active substances in organisms
The investigation deals with the affection of permeation of mupirocin from the Bactroban® Leciva ointment through full-thickness pig ear skin by alaptide that was applied in micronized or nanonized form as a potential excipient
Mupirocin was chosen as a frequently applied antibiotic for topical treatment of bacterial skin infections that are often associated with various injuries of the skin, because alaptide itself showed significant curative effect on the skin [17,25]

Summary

Introduction

Development in the field of pharmaceutical dosage forms results in the discovery of additional highly sophisticated drug delivery systems that allow for the maintaining of constant levels of active substances in organisms. The investigation deals with the affection of permeation of mupirocin from the Bactroban® Leciva ointment through full-thickness pig ear skin by alaptide that was applied in micronized or nanonized form as a potential excipient. Rapid primary screening showed that the two forms of alaptide differently influenced 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.

Results

Conclusion