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 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.

Participation and Drug Resistance of Coagulase-Positive Staphylococci Isolated From Cases of Pyoderma and Otitis Externa in Dogs

“…In the present study, all multi-drug resistant strains were susceptible to mupirocin, and zones of growth inhibition (> 19 mm at the 5 μg disc) were in agreement with Creagh and Lucey (33). Mupirocin (mixture of several pseudomonic acids) is an antibiotic originally isolated from Pseudomonas fluorescens and is structurally unrelated to any other antibiotic (34). Pseudomonic acid is capable of binding to the isoleucyl t-RNA synthetase in Staphylococcus sp., resulting in a total inhibition of their protein synthesis (35).…”

“…Unfortunately, after intravenous or oral administration, mupirocin is rapidly metabolized to monic acid, which has no antibacterial activity. Therefore, only topical treatment of bacterial skin infections (as ointments or creams) or nano-carriers remain available (34).…”