Modulation of the barrier function of the skin

Modulation of the barrier function of the skin
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DOI:
10.1159/000056393
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发表时间:
2001-01-01
期刊:
SKIN PHARMACOLOGY AND APPLIED SKIN PHYSIOLOGY
影响因子:
--
通讯作者:
Hadgraft, J
Hadgraft, J
中科院分区:
其他
文献类型:
--
作者:
Hadgraft, J

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外源性物质穿过角质层(皮肤的速率控制膜)的运输很慢,而且机制似乎很复杂。然而,基本的转移是由基本的物理化学概念控制的,其中主要的是分配(K),扩散(D)和溶解度(C-s)。因此,为了改变渗透率,显然应该以这些参数为目标。在大多数情况下,采用增强策略来改善D、K或C-s,然而,存在渗透减少可能是有益的情况。实例包括防晒剂或驱虫剂的局部应用。该出版物展示了调制效应的评估方法以及确定哪些物理化学参数受到影响的困难。如果配方影响一种以上,则通常可以看到协同作用。计算机建模的进展提供了一个深入了解一些化学增强剂在分子水平上的作用机制。已经报道了用于递送大分子如胰岛素(与传递体相关)或DNA(作为DOTAP复合物)的增强的皮肤吸收。为了实现这一点,必须调节皮肤的阻隔性能。然而,确切的作用机制尚未阐明。版权所有(C)2001 S. Karger AG,巴塞尔。
Transport of xenobiotics across the stratum corneum, the rate-control ling membrane of skin, is slow and the mechanism appears complex. However, the basic transfer is controlled by fundamental physicochemical concepts, the predominant of which are partition (K), diffusion (D) and solubility (C-s). In order to change the rate of penetration it is therefore clear that it is these parameters that should be targeted. In most instances enhancement strategies are adopted to improve D, K or C-s, however there are instances in which permeation reduction may be beneficial. Examples include the topical application of sunscreens or insect repellents. This publication demonstrates the way in which modulation effects can be assessed and the difficulties involved in determining which of the physicochemical parameter(s) are being affected. If the formulation influences more than one, synergism can often be seen. Advances in computer modelling have provided an insight into the mechanisms of action of some of the chemical enhancers at a molecular level. Enhanced skin absorption has been reported for the delivery of macromolecules such as insulin (associated with transfersomes) or DNA (as a DOTAP complex). The barrier property of the skin must be modulated for this to be achieved. However the precise mechanisms of action have not been elucidated. Copyright (C) 2001 S. Karger AG, Basel.