title: Measurement, analysis and prediction of topical UV filter bioavailability.
abstract: The aim of the present study was to objectively quantify and predict bioavailability of three sunscreen agents (i.e., benzophenone-3, 2-ethylhexylsalicylate, and 2 ethylhexyl-4-methoxycinnamate) in epidermis treated by petrolatum and emulsion-based formulations for 7 and 30min on four human volunteers. Profiles of sunscreen agents through stratum corneum (SC), derived from the assessment of chemical amounts in SC layers collected by successive adhesive tape-stripping, were successfully fitted to Fick's second law of diffusion. Therefore, permeability coefficients of sunscreen agents were found lower with petrolatum than with emulsion based formulations confirming the crucial role of vehicle in topical delivery. Furthermore, the robustness of that methodology was confirmed by the linear relationship between the chemical absorption measured after 30min and that predicted from the 7-min exposure experiment. Interestingly, in this dermatopharmacokinetic method, the deconvolution of permeability coefficients in their respective partition coefficients and absorption constants allowed a better understanding of vehicle effects upon topical bioavailability mechanisms and bioequivalence of skin products.
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France.
authors.forename: L
authors.initials: L
authors.lastname: Roussel
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France.
authors.forename: E
authors.initials: E
authors.lastname: Gilbert
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France.
authors.forename: D
authors.initials: D
authors.lastname: Salmon
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France.
authors.forename: C
authors.initials: C
authors.lastname: Serre
authors.affiliation: Iderma, Dornacherstrasse 324, CH-4053 Basel, Switzerland.
authors.forename: B
authors.initials: B
authors.lastname: Gabard
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France.
authors.forename: M
authors.initials: M
authors.lastname: Haftek
authors.affiliation: Department of Dermatology, Box 0989, University of California San Francisco, CA 94143-0989, USA.
authors.forename: H I
authors.initials: HI
authors.lastname: Maibach
authors.affiliation: Université Lyon 1, EA 4169 Fundamental, Clinical and Therapeutic Aspects of the Skin Barrier Function, SFR Lyon-Est Santé, Lyon, France. Electronic address: fabrice.pirot@univ-lyon1.fr.
authors.forename: F
authors.initials: F
authors.lastname: Pirot
mesh_terms: D000287:Administration, Topical; D000328:Adult; D000368:Aged; D001577:Benzophenones / Q000493:pharmacokinetics*; D001682:Biological Availability; D002934:Cinnamates / Q000493:pharmacokinetics*; D006801:Humans; D008875:Middle Aged; D012459:Salicylates / Q000493:pharmacokinetics*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013473:Sunscreening Agents / Q000493:pharmacokinetics*
chemical_list: D001577:Benzophenones; D002934:Cinnamates; D012459:Salicylates; D013473:Sunscreening Agents; C103422:2-ethylhexyl salicylate; C118580:octylmethoxycinnamate; C005290:oxybenzone
keywords: Bioequivalence; Chemical UV filters; Dermatopharmacokinetics; Topical bioavailability