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The Effect of Two Azones on the Lateral Lipid Organization of Human Stratum Corneum and Its Permeability

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Abstract

Purpose. Investigation of the relationship between changes in humanSC lipid organization induced by N-alkyl-azocycloheptane-2-one andSC permeability to the model compound HgCl2.

Methods. Human dermatomed skin was treated with propylene glycol(PG), oleyl-Azone (OAz) or dodecyl-Azone (DAz) in 0.15 M PG.Untreated skin served as control. The lateral lipid organization wasstudied by electron diffraction. Hg was measured on tape-strips by X-raymicroanalysis and in the acceptor phase by atom absorptionspectrometry.

Results. In control and PG treated samples, the lipid packing wasmainly orthorhombic, while a small fraction was hexagonal. In OAz andDAz treated samples, the orthorhombic lipid organization remained,however, the hexagonal packing was recorded less frequently. Theamount of Hg decreased as a function of depth in all SC samples,however, the penetration profile increased significantly upon OAztreatment. The cumulative amount of Hg in the acceptor phase of OAztreated samples also increased significantly compared to control andPG treated samples.

Conclusions. The increased penetration of Hg into OAz treated skincould not be related to an orthorhombic-hexagonal phase transition.Alternatively, phase separation of OAz and/or formation of grainboundaries might affect SC permeability, hereby increasing Hgpenetration. A similar mechanism is proposed for DAz.

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Authors and Affiliations

  1. Center for Electron Microscopy, Leiden University Medical Center, P.O. Box 9503, 2300 RA, Leiden, The Netherlands

    Gonneke S. K. Pilgram

  2. Center for Electron Microscopy, Leiden University Medical Center, P.O. Box 9503, 2300 RA, Leiden, The Netherlands

    A. Marjolein Engelsma-van Pelt & Henk K. Koerten

  3. Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9502, 2300 RA, Leiden, The Netherlands

    Joke A. Bouwstra

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  1. Gonneke S. K. Pilgram
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Pilgram, G.S.K., Engelsma-van Pelt, A.M., Koerten, H.K. et al. The Effect of Two Azones on the Lateral Lipid Organization of Human Stratum Corneum and Its Permeability. Pharm Res 17, 796–802 (2000). https://doi.org/10.1023/A:1007547906856

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