Caco-2 monolayers in experimental and theoretical predictions of drug transport

This review examines the use of Caco-2 monolayers in the prediction of inte stinal drug absorption. First, the different routes of drug transport in Ca co-2 monolayers are compared with those seen in vivo. Second, the predictio n of drug absorption in vivo from transport experiments in cell monolayers is discussed for different classes of drugs. Finally, the use of Caco-2 mon olayers as a reference model in physico-chemical and theoretical prediction s of drug absorption is discussed. We conclude that Caco-2 monolayers can b e used to identify drugs with potential absorption problems, and possibly a lso to select drugs with optimal passive absorption characteristics from se ries of pharmacologically active molecules generated in drug discovery prog rams. (C) 2001 Elsevier Science B.V. All rights reserved.