Uptake and desorption of hydrophilic compounds from human stratum corneum

JOURNAL OF CONTROLLED RELEASE

卷:261

Article

Miller, Matthew A.¹  Yu, Fang²  Kim, Keun-il³  Kasting, Gerald B.¹ 

[1] Univ Cincinnati, James L Winkle Coll Pharm, Cincinnati, OH USA

[2] Univ Cincinnati, Coll Engn & Appl Sci, Cincinnati, OH USA

[3] Univ Cincinnati, Dept Chem, Coll Arts & Sci, Cincinnati, OH USA

关键词: Desorption;    Diffusion;    Mathematical model;    Skin;    Stratum corneum;    Transport;   

DOI  :  10.1016/j.jconrel.2017.06.015

来源: Elsevier

【 摘 要 】

Small, polar compounds, both ionic and uncharged, partition into human stratum corneum immersed in aqueous solutions to an extent comparable to the water volume fraction of the tissue, then desorb in two phases. The fast phase has a time constant on the order of a few minutes, whereas the slow phase occurs over many hours. A physical model for this behavior involving a combination of tranverse diffusion through the tissue and lateral diffusion and exchange with skin appendages is presented. This concept is probed using excised human stratum corneum exposed to aqueous solutions of radiolabeled sodium chloride, tetraethyl ammonium bromide and mannitol, plus previously published data on six other compounds of varying molecular size and polarity. The fast phase desorption process becomes unimportant for lipophilic compounds. Slow phase desorption rates are size-selective, with larger species desorbing much more slowly than smaller ones. Interpreting the size-selectivity in terms of smooth cylindrical pores using the centerline approximation leads to an optimum pore radius of about 8-12 angstrom, depending on the model chosen.

【 授权许可】

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