In vivo Determination of the Diclofenac Skin Reservoir: Comparison between passive, occlusive and iontophoretic Application

Clijsen, Ron and Baeyens, Jean Pierre and Barel, André Odilon and Clarys, Peter (2015) In vivo Determination of the Diclofenac Skin Reservoir: Comparison between passive, occlusive and iontophoretic Application. Drug Design, Development and Therapy, 9. pp. 835-840. (In Press)

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Aim: There is scarce information concerning the pharmacodynamic behavior of topical substances used in the physiotherapy setting. Aim of the present study was to estimate the formation and emptying of the diclofenac (DF) skin reservoir after passive, semi occlusive and electrically assisted applications of DF. Methods: Five different groups of healthy volunteers (ntotal= 60; 23 male and 37 female), participated in this study. A 1% DF (Voltaren® Emulgel®, Novartis Pharma, Bern, Switzerland) formulation (12mg) was applied on the volar forearms on randomized defined circular skin areas of 7cm2. DF was applied for 20 minutes under 3 different conditions at the same time. Presence of DF in the skin results in a reduction of the methyl nicotinate (MN) response. To estimate the bioavailability of DF in the skin, MN responses at different times following initial DF application (respectively 1.5, 6, 24, 32, 48, 72, 96, 120 hours) were analysed. Results: At 1.5 hours after the initial DF application a significant decrease in the MN response was detected for the occluded and iontophorectical delivery. Passive application resulted in a decrease of the MN response from 6 hours post DF application. The inhibition remained up to 32 hours post DF application for the iontophoretic delivery; 48 hours for the occluded application; and 72 for the passive delivery. At 96 and 120 hours post DF application none of MN responses were inhibited. Conclusion: The formation and emptying of a DF skin reservoir was found to be dependent of the DF application mode. Penetration enhanced delivery resulted in a faster emptying of the reservoir. Keywords: transdermal drug delivery, passive diffusion, occlusion, iontophoresis, Diclofenac

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