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首页> 外文期刊>Journal of applied toxicology >Stratum corneum reservoir as a predictive method for in vitro percutaneous absorption
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Stratum corneum reservoir as a predictive method for in vitro percutaneous absorption

机译：角质层储层作为体外经皮吸收的预测方法

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Interaction between drug and proteins and lipids in stratum corneum (SC) is an important pharmacokinetic parameter in early steps of absorption. Previous in vivo studies showed that the total amount of compound, regardless of properties, penetrating over a 96h period could be predicted by the amount present in SC 30min after application by a linear relationship. Validating this linear relationship through in vitro study would facilitate testing of transdermal drug delivery platforms. We aimed to determine in vitro penetration behavior across SC of humans by determining the relationship between quantity present in SC reservoir 30min after application with 24h skin absorption and penetration. In this study, use of the SC reservoir effect to predict absorption and penetration of topical compounds is reaffirmed with in vitro models involving human skin. These results indicate the amount in short-term (30min) SC reservoir predict long-term (24h) skin absorption and penetration, as characterized by statistically significant linear relationships determined via regression. This may be explained by the fact that SC is a rate-limiting barrier to percutaneous drug transport. After molecules diffuse through SC barrier, passage into deeper dermal layers and systemic uptake occur relatively quickly. These results enable one to measure quantity in SC reservoir shortly after topical application as a proxy for absorption and penetration over longer periods. With respect to drug development and risk assessment of toxic substances, this may simplify assays attempting to quantitate penetration capacity. Further investigation with a larger range of compounds is needed to clarify the observations recorded here. Copyright (c) 2015 John Wiley & Sons, Ltd.
机译：药物与角质层（SC）中的蛋白质和脂质之间的相互作用是吸收早期的重要药代动力学参数。先前的体内研究表明，化合物的总量（不考虑其性质）在96小时内的渗透率都可以通过施用后30分钟内SC的线性关系来预测。通过体外研究验证这种线性关系将有助于测试透皮给药平台。我们的目的是通过测定24小时皮肤吸收和渗透后30分钟内SC储库中存在的数量之间的关系，从而确定跨人SC的体外渗透行为。在这项研究中，涉及人体皮肤的体外模型再次证实了使用SC储库效应预测局部化合物的吸收和渗透的作用。这些结果表明，短期（30分钟）SC储层中的量可预测长期（24小时）皮肤吸收和渗透，其特征在于通过回归确定的统计学上显着的线性关系。这可能是由于SC是经皮药物运输的限速屏障。分子通过SC屏障扩散后，进入较深的真皮层并全身吸收相对较快。这些结果使人们能够在局部应用后不久测量SC储层中的数量，以作为较长时期内吸收和渗透的代理。关于药物开发和有毒物质的风险评估，这可以简化试图量化渗透能力的测定。需要对更大范围的化合物进行进一步研究，以澄清此处记录的观察结果。版权所有（c）2015 John Wiley＆Sons，Ltd.

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