Bile secretion serves different important functions. First, it is one of th
e main mechanisms for the disposition of many endogenous and exogenous amph
ipatic compounds, including drugs, toxins, and waste products. Second, it s
upplies bile salts to the intestine, which is of crucial importance for the
emulsification of dietary, lipids. In the last decade considerable progres
s has been achieved in the elucidation of the process of bile formation. Se
veral key transporters in the canalicular membrane have been identified and
characterized This also holds for the mechanism of biliary lipid secretion
, where the lipid translocating function of a P-glycoprotein was found to b
e indispensable for phospholipid secretion. Concomitantly, it became clear
that bile salt-induced lipid secretion is an extremely complex process, in
which several steps remain elusive. The production of mice with a specific
defect in bilary lipid secretion and the identification of an analogous inh
erited human disease have made it possible to study the integrated function
of biliary lipid secretion in whole body lipid homeostasis. In this review
we discuss our current understanding of hepatocanalicular lipid secretion
in this context. The pathologic consequences of defects in biliary lipid se
cretion are discussed in another review in this issue.