From interaction of lipidic vehicles with intestinal epithelial cell membranes to the formation and secretion of chylomicrons.

Lipophilic drugs are carried by chylomicrons that are secreted by the small intestine and transported in lymph. This review discusses the digestion, uptake, and transport of dietary lipids and the impact that these processes have on the absorption of lipophilic drugs by the gastrointestinal tract. This chapter complements Dr. Chris Potter's chapter on the "pre-absorptive" events of drug processing and solubilization. This chapter reviews the digestion of lipids in the gastric and intestinal lumen and the role of bile salts in the solubilization of lipid digestion products for uptake by the gut. Both the passive and active uptake of lipid digestion products is discussed. How intestinal lipid transporters located at the brush border membrane may play a role in the uptake of lipids by the enterocytes is examined, as is the regulation of the absorption of cholesterol by the human ATP-binding cassette transporter-1 (ABC1). The intracellular trafficking and the resynthesis of complex lipids from lipid digestion products are explored, and the formation and secretion of chylomicrons are described.