The liver is responsible for the detoxification and biliary excretion
of a variety of endogenous and xenobiotic compounds and therefore, is
capable of responding to rapid fluctuations in metabolic demand. In or
der to accomplish this function, the hepatocyte must efficiently trans
port a host of substrates with wide-ranging physical-chemical properti
es to intracellular sites for biotransformation and subsequent secreti
on into the bile. The trafficking of substrates and metabolites within
the liver cell is a complex process, involving the coordinated action
of cellular proteins, organellar membranes, the cytoskeleton, vesicul
ar transport pathways, and bulk convective cytoplasmic flow. This revi
ew summarizes recent developments in the field of intracellular transp
ort, with particular reference to the metabolism of small hydrophobic
and amphipathic molecular species (e.g., bilirubin, bile salts, fatty
acids) by the hepatocyte.