The effect of urea and taurine as hydrophilic penetration enhancers on stratum corneum lipid models
The effect of urea and taurine as hydrophilic penetration enhancers on stratum corneum lipid models
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DOI：
10.1016/j.bbamem.2016.05.010
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发表时间：
2016-09-01
影响因子：
3.4
通讯作者：
Neubert, R. H. H.
中科院分区：
文献类型：
--
作者：
Mueller, J.;Oliveira, J. S. L.;Neubert, R. H. H.
为了优化药物的透皮应用，需要可逆地降低皮肤，特别是角质层（SC）的屏障功能。为此，应用渗透促进剂如尿素或牛磺酸。到目前为止，尚不清楚这种渗透增强是由与SC脂质基质的相互作用引起的还是与角质细胞内的作用有关。因此，这两种亲水性增强剂对不同维度的SC模型的影响，从单层到多层，在这项研究中进行了研究。许多复杂的方法被应用于确定这两种物质在分子尺度上的作用模式。实验表明，当10%尿素或5%牛磺酸溶液加入SC模型系统时，没有特异性相互作用。没有额外的水吸收的头基区域和没有减少的脂质链堆积密度已被观察到。因此，我们假设这两种物质的渗透增强作用可能是基于将大量水引入角质细胞，这是由尿素的巨大水结合能力和牛磺酸情况下产生的渗透压引起的。(C)2016爱思唯尔B.V.保留所有权利。
To optimize transdermal application of drugs, the barrier function of the skin, especially the stratum corneum (SC), needs to be reduced reversibly. For this purpose, penetration enhancers like urea or taurine are applied. Until now, it is unclear if this penetration enhancement is caused by an interaction with the SC lipid matrix or related to effects within the corneocytes. Therefore, the effects of both hydrophilic enhancers on SC models with different dimensionality, ranging from monolayers to multilayers, have been investigated in this study. Many sophisticated methods were applied to ascertain the mode of action of both substances on a molecular scale. The experiments reveal that there is no specific interaction when 10% urea or 5% taurine solutions are added to the SC model systems. No additional water uptake in the head group region and no decrease of the lipid chain packing density have been observed. Consequently, we suppose that the penetration enhancing effect of both substances might be based on the introduction of large amounts of water into the corneocytes, caused by the enormous water binding capacity of urea and a resulting osmotic pressure in case of taurine. (C) 2016 Elsevier B.V. All rights reserved.