ABSTRACT
The transport of orally-administered lipophilic drugs and xenobiotics into the systemic circulation relies, at least partially, on association with intestinal chylomicrons (CM) followed by lymphatic transport to the venous blood supply. This review discusses the digestion, uptake, and transport of dietary lipids by both passive and active processes, the role of bile salts in the solubilization of lipid digestion products and the impact these processes have on the absorption of lipophilic drugs and xenobiotics by the gastrointestinal tract. Finally, the intracellular trafficking and the resynthesis of complex lipids from lipid digestion products are explored, and the formation and secretion of CM are described. This chapter is intended to complement the discussion appearing elsewhere in this book describing the use of preclinical data to guide formulation development strategies for poorly water-soluble drugs.
