title: Ex vivo Cutaneous Bioavailability of Topical Mometasone Furoate in an O/W Preparation.
abstract: Mometasone furoate (MMF) is a modern glucocorticoid of the 4th generation, which has been proven not only for inhalation but also for cutaneous treatment. Due to its lipophilic character, it is mainly used in ointments and creams with an outer lipophilic phase (W/O type). However, this study investigated the cutaneous cytotoxicology of MMF and tried to characterize its pharmacokinetic effects on the skin using an O/W preparation. An HPLC method has been developed and validated for the detection of MMF in cutaneous tissue, and concentration-time curves of MMF were created after cutaneous application on unaffected as well as lesional skin. Cytotoxicological characterization was carried out using scratch assays on keratinocytes and cutaneous fibroblasts. Results showed that the condition of the skin had no significant impact on the cutaneous bioavailability of MMF, but the intrinsic effect of the O/W vehicle could be utilized in periods of acute inflammation. Cytotoxicological data gave no new indications regarding the safety of MMF.
authors.affiliation: Department of Dermatology and Venereology, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.
authors.forename: Johannes
authors.initials: J
authors.lastname: Wohlrab
authors.forename: Reinhard H H
authors.initials: RH
authors.lastname: Neubert
authors.forename: Elfi
authors.initials: E
authors.lastname: Sommer
authors.forename: Julia
authors.initials: J
authors.lastname: Michael
mesh_terms: D000279:Administration, Cutaneous; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D005347:Fibroblasts / Q000187:drug effects; D005938:Glucocorticoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects; D000068656:Mometasone Furoate / Q000008:administration & dosage / Q000493:pharmacokinetics*; D009821:Oils; D012867:Skin / Q000187:drug effects / Q000378:metabolism*; D063465:Skin Cream / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014867:Water
chemical_list: D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D009821:Oils; D000068656:Mometasone Furoate; D014867:Water