CACO-2 MONOLAYERS IN EXPERIMENTAL AND THEORETICAL PREDICTIONS OF DRUGTRANSPORT

This review examines the use of Caco-2 monolayers in the prediction of intestinal drug absorption. First, the different routes of drug trans port 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. Final ly, the use of Caco-2 monolayers as a reference model in physico-chemi cal and theoretical predictions of drug absorption is discussed. We co nclude that Caco-2 monolayers can be used to identify drugs with poten tial absorption problems, and possibly also to select drugs with optim al passive absorption characteristics from series of pharmacologically active molecules generated in drug discovery programs.