Drug Delivery 2015-01-01

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

Sara Raposo, Rita Tavares, Lídia Gonçalves, Sandra Simões, Manuela Urbano, Helena M Ribeiro

Index: Drug Deliv. 22 , 562-72, (2015)

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Abstract

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 in vitro and in vivo 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). In vitro 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(-4 )cm/h to 5.20 × 10(-4) ± 2.05 × 10(-4 )cm/h and 6.30 × 10(-4) ± 2.94 × 10(-4 )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 stratum corneum (SC) was 10.61%. The in vivo 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.