Studying the effectiveness of penetration enhancers to deliver retinol through the stratum cornum by in vivo confocal Raman spectroscopy
Studying the effectiveness of penetration enhancers to deliver retinol through the stratum cornum by in vivo confocal Raman spectroscopy
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DOI：
10.1016/j.jconrel.2009.04.023
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发表时间：
2009-08-19
影响因子：
10.8
通讯作者：
Puppels, Gerwin J.
中科院分区：
文献类型：
--
作者：
Melot, Mickael;Pudney, Paul D. A.;Puppels, Gerwin J.
本研究的目的是监测体内化学渗透增强剂对反式视黄醇输送到人体皮肤的影响。化学渗透增强剂通过破坏膜结构或最大化药物在皮肤中的溶解度来可逆地改变 SC 的屏障特性。迄今为止，大多数渗透或渗透实验都是在体外进行的。拉曼光谱具有独特的能力，能够测量体内的生物过程，本文首次表明，使用该技术可以成功地在体内测量渗透增强剂对反式视黄醇输送的影响。在这里，志愿者的掌侧前臂接受了四种制剂的治疗。一种配方是从离体实验中鉴定出的高效模型递送系统：丙二醇 (PC)/乙醇中的反式视黄醇，其中 PG 是众所周知的高效渗透促进剂。其他三种配方基于辛酸/癸酸甘油三酯 (MYRITOL(R)318) 中的 0.3% 反式视黄醇，这是一种常用于护肤霜的油，但其中两种配方添加了特定的渗透促进剂。一种配方含有脂质提取剂 Triton X 100，而另一种配方含有脂质流化剂油酸。溶液施用一次并在处理后 6 小时内进行测量。可以清楚地看到含有或不含有渗透促进剂的制剂之间反式视黄醇的递送的显着差异。此外，渗透促进剂的类型也被证明会影响递送。使用油酸（一种脂质流化剂）时，可以检测到反式视黄醇在皮肤中的更好输送。首次在体内非侵入性地随时间监测渗透促进剂对反式视黄醇递送的影响。 (C) 2009 Elsevier B.V. 保留所有权利。
The purpose of this study is to monitor in vivo the effect of chemical penetration enhancers on the delivery of trans-retinol into human skin. Chemical penetration enhancers reversibly alter barrier properties of the SC by disruption of the membrane structures or maximising drug solubility with the skin. So far, most of permeation or penetration experiments are performed in vitro. Raman spectroscopy is uniquely placed to be able to measure biological processes in vivo and this paper shows for the first time that the effect of penetration enhancer on the delivery of trans-retinol can successfully be measured in vivo using this technique. Here, the volar forearm of volunteers was treated with four formulations. One formulation is a highly effective model delivery system identified from ex vivo experiments: trans-retinol in Propylene Glycol (PC)/ethanol, with PG being a well-known and efficient penetration enhancer. The other three formulations are based on 0.3% trans-retinol in Caprylic/Capric Acid Triglyceride (MYRITOL(R)318), an oil commonly used in skin creams but in two of them a specific penetration enhancer is added. One contains a lipid extractor, Triton X 100, whereas another formulation contains a lipid fluidiser, Oleic Acid. Solutions were applied once and measurements were performed up to 6 h after treatment. Remarkable differences in the delivery of trans-retinol between formulation with or without penetration enhancer can clearly be seen. Moreover, the type of penetration enhancer is also shown to influence the delivery. While using the Oleic Acid, which is a lipid fluidiser, a better delivery of trans-retinol in the skin can be detected. For the first time, the effect of penetration enhancer on the delivery of trans-retinol has been monitored, non invasively in vivo, with time. (C) 2009 Elsevier B.V. All rights reserved.