Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers
Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers
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DOI：
10.1038/nprot.2007.303
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发表时间：
2007-01-01
期刊：
影响因子：
14.8
通讯作者：
Artursson, Per
中科院分区：
文献类型：
--
作者：
Hubatsch, Ina;Ragnarsson, Eva G. E.;Artursson, Per
在渗透性支持物上培养的人结肠癌细胞系 Caco-2 单层的渗透性系数通常用于预测口服药物和其他异生物质的吸收。该协议描述了我们在 Caco-2 模型中培养、表征和测定异生物质（通常是类药物化合物）渗透系数的方法。多年来引入的一些修改已纳入协议中。该方法可用于追踪测试化合物在两个方向上的渗透性，从顶端到基底外侧，反之亦然，并且可以研究被动和主动运输过程。如果Caco-2单层细胞提前3周在渗透性支持物上培养和分化，渗透性测定可在1个工作日内完成。
Permeability coefficients across monolayers of the human colon carcinoma cell line Caco-2, cultured on permeable supports, are commonly used to predict the absorption of orally administered drugs and other xenobiotics. This protocol describes our method for the cultivation, characterization and determination of permeability coefficients of xenobiotics (which are, typically, drug-like compounds) in the Caco-2 model. A few modifications that have been introduced over the years are incorporated in the protocol. The method can be used to trace the permeability of a test compound in two directions, from the apical to the basolateral side or vice versa, and both passive and active transport processes can be studied. The permeability assay can be completed within one working day, provided that the Caco-2 monolayers have been cultured and differentiated on the permeable supports 3 weeks in advance.