文章基本信息

标题：Penetration of Ufenamate into Intact, Stripped, or Delipidized Skin Using Different Vehicles
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作者：Hayato Iino ; Makiko Fujii ; Manami Fujino 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2015
卷号：38
期号：10
页码：1645-1648
DOI：10.1248/bpb.b15-00267
出版社：The Pharmaceutical Society of Japan
摘要：The purpose of this study was to clarify the effect of skin condition on skin penetration of the very high lipophilic drug, ufenamate (UF). UF was applied to stripped or delipidized skin using liquid paraffin (LP) or purified water containing polysorbate 80 at a dose of 2 µL/cm². We found that UF penetration into intact and stripped skin using a water vehicle was respectively 5 and 10 times higher than that using LP. UF is freely soluble in oil and insoluble in water; thus, activity in water is higher than that in LP. Therefore, it is useful to use a water-based vehicle for both intact sites and those with defective stratum corneum (SC). Conversely, we found that delipidization of SC decreased the penetration of UF significantly with both LP and water, and the amount measured in the epidermis was 1 µg/cm² with both vehicles. This indicates that UF is not suitable for so-called “dry skin.” This study revealed clinically relevant differences in the penetration of UF into intact, stripped, or delipidized skin conditions.