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Intestinal lipid absorption processes encompass the complex physiological sequence by which dietary fats, including triglycerides, cholesterol, and phospholipids, are digested and transported from the intestinal lumen into the bloodstream. This multi-step pathway involves emulsification by bile salts, enzymatic hydrolysis by lipases, micellar transport to the enterocyte brush border, and protein-mediated uptake via transporters such as NPC1L1 and CD36. Once inside the enterocyte, lipids are re-esterified and packaged into chylomicrons through the action of enzymes like DGAT and the assembly protein MTP before being secreted into the lymphatic system. Because excessive lipid absorption is a primary driver of hyperlipidemia and cardiovascular disease, various components of this process serve as therapeutic targets. Drugs like ezetimibe and orlistat modulate these processes to lower systemic lipid levels, though they often carry side effects related to gastrointestinal malabsorption.
Inhibition of specific enzymes (e.g., gastric and pancreatic lipases), transporters (e.g., NPC1L1), or intracellular assembly proteins (e.g., MTP) to reduce the entry of dietary fats and cholesterol into the systemic circulation.
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