ADMET and DMPK, Vol. 2 No. 1, 2014.
Original scientific paper
https://doi.org/10.5599/admet.2.1.26
Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide
Radka Opatrilova
; Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic
Josef Jampilek
orcid.org/0000-0003-2003-9052
; Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic
Abstract
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. Alaptide, (S)-8-methyl-6,9-diazaspiro[4.5]decan-7,10-dione, was the original Czech compound. It was discovered 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 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.
Keywords
alaptide; mupirocin; nanoparticles; Bactroban®
Hrčak ID:
119020
URI
Publication date:
1.4.2014.
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