There are several possible approaches that can be used to increase the
oral absorption of drugs. Recently, utilization of carrier-mediated t
ransport mechanisms in the intestinal tract to increase the bioavailab
ility of drugs has drawn a great deal of attention. This review descri
bes the potential use of this approach, using the bile acid carrier sy
stem in both the intestinal tract and the Ever. The physiology; ontoge
ny and molecular biology of the ileal and hepatic transporters are des
cribed and an overview is presented of the compounds that are transpor
ted by these carriers. Furthermore, the structural requirements for re
cognition by these carrier systems is presented and the current Utiliz
ation of this mechanism is reviewed. The importance of carrier-mediate
d bile acid transport in drug delivery is addressed.