Non-invasive assessment of the effect of formulation excipients on stratum corneum barrier function in vivo
Non-invasive assessment of the effect of formulation excipients on stratum corneum barrier function in vivo
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DOI：
10.1016/j.ijpharm.2003.11.016
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发表时间：
2004-03-01
影响因子：
5.8
通讯作者：
Guy, RH
中科院分区：
文献类型：
--
作者：
Curdy, C;Naik, A;Guy, RH
本工作的目的是研究制剂辅料对体内人角质层（SC）屏障功能的影响。在封闭和非封闭条件下，将两种制剂（软膏和水包油乳膏）施用于人类志愿者的皮肤。然后使用三种非侵入性生物物理技术评估每种治疗的效果：经表皮水分损失（TEWL），阻抗谱（IS）和衰减全反射傅里叶变换红外（ATR-FTIR）光谱。这些测量与简单的胶带剥离方案相结合，以允许在整个SC中获得信息。IS和TEWL提供了每种制剂对皮肤屏障功能影响的基本信息，而ATR-FTIR能够（i）跟踪制剂辅料并评价其在SC中的浓度分布，以及（ii）推导解释TEWL和IS结果的机制细节。结果发现，在存在或不存在乳膏的情况下皮肤的封闭导致TEWL增加，当处理在6小时终止时。另一方面，将软膏吸收到SC中抑制了应用后的TEWL率。与此同时，治疗与软膏引起的相对低频皮肤阻抗的增加，与额外的亲脂性成分进入SC一致。后者证实了ATR-FTIR光谱测量。总的来说，结合使用的三个生物物理测量允许配方的影响，并摄取到，SC进行推导和评估，该方法可能被证明是有用的，为未来的选择和优化的局部给药载体。(C)2003 Elsevier B. V.保留所有权利。
The objective of the present work was to investigate the effect of formulation excipients on human stratum corneum (SC) barrier function in vivo. Two formulations, an ointment and an oil-in-water cream, were applied to the skin of human volunteers under both occlusive and non-occlusive conditions. The effects of each treatment were then evaluated using three non-invasive biophysical techniques: transepidermal water loss (TEWL), impedance spectroscopy (IS) and attenuated-total-reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. These measurements were combined with a simple tape-stripping protocol to allow information to be derived across the entire SC. IS and TEWL provided basic information on the effect of each formulation on skin barrier function, while ATR-FTIR enabled (i) the tracking of formulation excipients and evaluation of their concentration profiles within the SC, and (ii) deduction of mechanistic detail with which to explain the TEWL and IS results. It was found that occlusion of the skin either in the presence or absence of the cream caused TEWL to be increased when the treatment was terminated at 6 h. Uptake of ointment into the SC, on the other hand, inhibited the post-application TEWL rate. In parallel, treatment with the ointment caused an increase in relative low-frequency skin impedance, consistent with the entry of additional lipophilic constituents into the SC. The latter was confirmed by ATR-FTIR spectroscopic measurements. Overall, the combined use of the three biophysical measurements allowed formulation effects on, and uptake into, the SC to be deduced and evaluated, and the approach may prove useful for the future selection and optimization of topical drug delivery vehicles. (C) 2003 Elsevier B.V. All rights reserved.