Comparison of the effects of chemical permeation enhancers on the lipoidal pathways of human epidermal membrane and hairless mouse skin and the mechanism of enhancer action

Comparison of the effects of chemical permeation enhancers on the lipoidal pathways of human epidermal membrane and hairless mouse skin and the mechanism of enhancer action
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DOI:
10.1002/jps.20865
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发表时间:
2007-09-01
影响因子:
3.8
通讯作者:
Higuchi, William I.
Higuchi, William I.
中科院分区:
医学3区
文献类型:
--
作者:
Chantasart, Doungdaw;Sa-Nguandeekul, Piyanuch;Higuchi, William I.

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以前,化学渗透促进剂对无毛小鼠皮肤(HMS)的脂质途径的渗透性的影响进行了研究,并建立了定量结构增强关系。本研究采用与以往人表皮细胞膜研究相同的实验方法,研究这些促进剂对人表皮细胞膜的作用。增强剂对皮质酮的HEM和HMS的类脂途径的渗透系数的影响被发现基本上是相同的。在增强剂和β-雌二醇的平衡摄取研究中,发现E = 10条件下吸收的增强剂的量和β-雌二醇分配到HEM角质层(SC)细胞间脂质中与HMS的那些不同。尽管存在这些差异,HEM数据显示增强子的细胞间脂质/PBS分配系数与增强子正辛醇/PBS分配系数之间存在相关性。这种相关性与先前研究中观察到的HMS SC中增强子作用位点的化学微环境一致。因此,提供适当的实验方案,HMS可以是一个可靠的模型,用于评估皮肤渗透促进剂对HEM的脂质途径的影响。(c)2007 Wiley-Liss,Inc.
Previously, the effects of chemical permeation enhancers upon the permeability of the lipoidal pathway of hairless mouse skin (HMS) were investigated and a quantitative structure enhancement relationship was established. The present study was to study the effects of these enhancers on human epidermal membrane (HEM) using the same experimental method employed in the previous HMS studies. The effects of enhancers on the permeability coefficients of the lipoidal pathways of HEM and HMS for corticosterone were found to be essentially the same. In the equilibrium uptake studies of the enhancers and beta-estradiol, it was found that the amounts of enhancers taken up and the partitioning of P-estradiol into the HEM stratum corneum (SC) intercellular lipid under the E = 10 conditions were different from those of HMS. Despite these differences, the HEM data show a correlation between the intercellular lipid/PBS partition coefficients of the enhancers and the enhancer n-octanol/PBS partition coefficients. This correlation is consistent with the observed chemical microenvironment of the site of enhancer action in the HMS SC in previous studies. Therefore, provided with proper experimental protocols, HMS can be a reliable model for the evaluation of the effects of skin permeation enhancers on the lipoidal pathway of HEM. (c) 2007 Wiley-Liss, Inc.