title: Mometasone furoate-loaded cold processed oil-in-water emulsions: in vitro and in vivo studies.
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.
authors.affiliation: Faculty of Pharmacy, Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), University of Lisbon , Lisbon , Portugal and.
authors.forename: Sara
authors.initials: S
authors.lastname: Raposo
authors.forename: Rita
authors.initials: R
authors.lastname: Tavares
authors.forename: Lídia
authors.initials: L
authors.lastname: Gonçalves
authors.forename: Sandra
authors.initials: S
authors.lastname: Simões
authors.forename: Manuela
authors.initials: M
authors.lastname: Urbano
authors.forename: Helena M
authors.initials: HM
authors.lastname: Ribeiro
mesh_terms: D000279:Administration, Cutaneous; D000293:Adolescent; D000328:Adult; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D004655:Emulsions; D005260:Female; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D051379:Mice; D008875:Middle Aged; D000068656:Mometasone Furoate / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D010539:Permeability; D012867:Skin / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D012869:Skin Absorption; D055815:Young Adult
chemical_list: D000893:Anti-Inflammatory Agents; D004655:Emulsions; D000068656:Mometasone Furoate
keywords: Cold process emulsion; epidermal targeting; glucocorticoids; reservoir effect; topical delivery