Development of Microsponges for Topical Delivery of Mupirocin

Abstract

The goal of the present study was to develop and evaluate microsponge-based topical delivery system of mupirocin for sustained release and enhanced drug deposition in the skin. Microsponges containing mupirocin were prepared by an emulsion solvent diffusion method. The effect of formulation and process variables such as internal phase volume and stirring speed on the physical characteristics of microsponges were examined on optimized drug/polymer ratio by 3(2) factorial design. The optimized microsponges were incorporated into an emulgel base. In vitro drug release, ex vivo drug deposition, and in vivo antibacterial activity of mupirocin-loaded formulations were studied. Developed microsponges were spherical and porous, and there was no interaction between drug and polymer molecules. Emulgels containing microsponges showed desired physical properties. Drug release through cellulose dialysis membrane showed diffusion-controlled release pattern and drug deposition studies using rat abdominal skin exhibited significant retention of active in skin from microsponge-based formulations by 24 h. The optimized formulations were stable and nonirritant to skin as demonstrated by Draize patch test. Microsponges-based emulgel formulations showed prolonged efficacy in mouse surgical wound model infected with S. aureus. Mupirocin was stable in topical emulgel formulations and showed enhanced retention in the skin indicating better potential of the delivery system for treatment of primary and secondary skin infections, such as impetigo, eczema, and atopic dermatitis.

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“…Emulgels containing microsponges showed desired physical properties. Drug release through cellulose dialysis membrane showed diffusion controlled release pattern and drug deposition studies using rat abdominal skin exhibited significant retention of active in skin from microsponge based formulations by 24 h 40 43 .…”

Toward Application of Microsponges in Transdermal Drug Delivery System

“…2 Additionally, TDDS permits the permeation of drugs across the skin and into the systemic circulation which avoids the hepatic first-pass effect observed in the course of oral administration and inconvenience of frequent parenteral administration. 3 As a new drug carrier of TDDS, Microsponges are mostly used for topical [4][5][6][7][8][9][10] and oral administration. [11][12][13][14][15] For other topical delivery systems, the traditional delivery systems are required of frequent dosing to keep relatively stable local concentrations of effective constituent for therapeutic effectiveness because of low effectiveness.…”

“…7 For this reason, as a porous polymeric microsphere, Microsponges can fulfill such aims uniquely. 4 Microsponges are porous, polymeric microspheres ( Figure 1) which are invariably used for topical delivery system; 4-5,7-10 its inside are full of lacunas and its particle size is 5~300μm in diameter. )…”

“…and MP emulgel (4.24±0.08)×(10 -3 cm·h -1 ), which showed that MS emulgel enhanced drug retention within the epidermis, and improved topical bioavailability. 7 (b) Non-irritation. The precious study carried out skin stimulant experiment using the New Zealand white rabbit, and the result showed no abnormality on the unbroken and damaged rabbit skin.…”

“…Thus, the result indicated that microsponges are non-irritational to the rabbit skin. 5,7 (c) Prolonged the duration of action of drug. In vitro drug release studies indicated that drug action duration of MP ointment (4-10h) and MP Emulgel (4-10h) are both shorter than that of MS emulgel (24h).…”