The relative effect of Azone(R) and Transcutol(R) on permeant diffusivity and solubility in human stratum corneum
The relative effect of Azone(R) and Transcutol(R) on permeant diffusivity and solubility in human stratum corneum
复制标题
DOI：
10.1023/a:1016037803128
复制
发表时间：
1996-04-01
影响因子：
3.7
通讯作者：
Brain, K
中科院分区：
文献类型：
--
作者：
Harrison, JE;Watkinson, AC;Brain, K
目的.本工作的目的是分析已知的促进剂Atone（R）和Transcutol（R）所证实的经皮渗透促进的机制。使用衰减全反射傅里叶变换红外光谱（ATR-FTIR）监测增强剂诱导的模型渗透物（4-氰基苯酚）在人角质层中的扩散率和溶解度的变化（体外），并与使用简单Franz型扩散池测量的增强剂对通量的总体影响进行比较。已经通过完善的Franz扩散池技术和使用ATR-FTIR光谱显示，所研究的增强剂都使氰基苯酚在体外穿过人皮肤的通量增加约两倍。此外，ATR-FTIR表明，这些增强剂可能通过不同的机制发挥作用。很可能Atone降低了角质层的扩散阻力，而Transcutol增加了渗透剂在此屏障中的溶解度。人们越来越关注某些增强剂似乎起作用的明显协同性质。虽然在目前的文献中有许多建议，但这些乘法和/或加法效应的确切性质尚不清楚。ATR-FTIR光谱的应用，这样的增强系统将允许所观察到的增强的机制进行更深入的探讨。
Purpose. The purpose of this work was to analyse the mechanism of the enhancement of percutaneous penetration demonstrated by the known enhancers Atone(R) and Transcutol(R).Methods. Enhancer induced changes in the diffusivity and solubility of a model permeant (4-cyanophenol) in human stratum corneum were monitored (in-vitro) using Attenuated total reflectance Fourier transform infra-red (ATR-FTIR) spectroscopy and compared to the gross effects of the enhancers on flux as measured using simple Franz-type diffusion cells.Results. It has been shown by both the well-established Franz diffusion cell technique and the use of ATR-FTIR spectroscopy that the enhancers studied both increase the flux of cyanophenol across human skin in-vitro by a factor of approximately two. Furthermore, it has been demonstrated by ATR-FTIR that these enhancers are likely to exert their effects by different mechanisms. It is probable that Atone reduces the diffusional resistance of the stratum corneum and that Transcutol increases the solubility of the penetrant in this barrier.Conclusions. There is increasing interest in the apparently synergistic nature in which certain enhancers appear to work. The exact nature of these multiplicative and/or additive effects is not known although there are numerous suggestions in the current literature. The application of ATR-FTIR spectroscopy to such enhancing systems will allow the mechanisms of the observed enhancements to be probed in greater depth.