Artursson P, Palm K, Luthman K
Department of Pharmaceutics, Uppsala Biomedical Centre, Uppsala University, Box 580, S-751 23, Uppsala, Sweden.
Adv Drug Deliv Rev. 2001 Mar 1;46(1-3):27-43. doi: 10.1016/s0169-409x(00)00128-9.
This review examines the use of Caco-2 monolayers in the prediction of intestinal drug absorption. First, the different routes of drug transport in Caco-2 monolayers are compared with those seen in vivo. Second, the prediction of drug absorption in vivo from transport experiments in cell monolayers is discussed for different classes of drugs. Finally, the use of Caco-2 monolayers as a reference model in physico-chemical and theoretical predictions of drug absorption is discussed. We conclude that Caco-2 monolayers can be used to identify drugs with potential absorption problems, and possibly also to select drugs with optimal passive absorption characteristics from series of pharmacologically active molecules generated in drug discovery programs.
本综述考察了Caco-2单层细胞在预测肠道药物吸收方面的应用。首先，将Caco-2单层细胞中不同的药物转运途径与体内观察到的途径进行比较。其次，针对不同类别的药物，讨论了根据细胞单层转运实验对体内药物吸收的预测。最后，探讨了Caco-2单层细胞在药物吸收的物理化学和理论预测中作为参考模型的应用。我们得出结论，Caco-2单层细胞可用于识别有潜在吸收问题的药物，也有可能从药物发现项目中产生的一系列药理活性分子中筛选出具有最佳被动吸收特性的药物。
