Mometasone furoate-loaded cold processed oil-in-water emulsions: in vitro and in vivo studies. (June 2015)

• Record Type: Journal Article
• Authors: Raposo, Sara; Tavares, Rita; Gonçalves, Lídia; Simões, Sandra; Urbano, Manuela; Ribeiro, Helena M.
• Is Part Of: Drug delivery. Volume 22:Number 4(2015:May)
• Page Start: 562
• Page End: 572
• Publication Date: 2015-06
• Subjects: Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2013.871086
• Languages: English
• ISSNs: 1071-7544

Abstract

<abstract> <title>Abstract</title> <p>Over the years, research has focused on strategies to increase benefit/risk ratio of corticoids. However, vehicles intended for topical glucocorticoids delivery with an improved benefit/risk ratio are still on demand. The aim of this work was the <italic>in vitro</italic> and <italic>in vivo</italic> characterization of cold processed oil-in-water (o/w) emulsions intended for mometasone furoate (MF) delivery to induce drug targeting to upper skin strata, decreasing adverse effects. Two o/w emulsions, containing 0.1% of MF, were developed differing in the glycol used (2-methyl-2, 4-pentanediol – PT and ethoxydiglycol – TC emulsions). <italic>In vitro</italic> permeation studies revealed that these emulsions are suitable vehicles for the delivery of MF containing ingredients which are responsible for a drastically increased on the permeability coefficients of MF from a theoretical value of 1.18 × 10<sup>−4 </sup>cm/h to 5.20 × 10<sup>−4</sup> ± 2.05 × 10<sup>−4 </sup>cm/h and 6.30 × 10<sup>−4</sup> ± 2.94 × 10<sup>−4 </sup>cm/h, for PT and TC, respectively. The tape stripping results showed that the amount of drug that reached the viable skin layers was very low (1.99 %) and the amount that remained in the <italic>stratum corneum</italic> (SC) was 10.61%. The <italic>in vivo</italic> studies showed that the developed formulations decreased the edema and erythema in mice skin in more that 90%, assuring, at least, the same anti-inflammatory effect compared with the commercial cream. PT placebo demonstrated to contribute to restore the skin barrier by increasing the amount of lipids within the human skin.</p> </abstract>