Liposome-based delivery system for effective chylomicron-mediated drug exocytosis in the intestinal cell monolayers

Abstract

When drugs are orally administered, drugs can be transported via either portal vein or lymphatic vessel. In case of portal vein route, the concentration of a drug is greatly reduced in the liver before it reaches the systemic circulation. However, lymphatic transport of a drug can bypass the first-pass metabolism in the liver and significantly enhance bioavailability. After exogenous lipids are absorbed into enterocytes, lipids are transformed to chylomicrons. Chylomicron exocytoses from the enterocyte and enters the lymphatic route. To enter the intestinal lymphatic system, we use liposomal formulation. Furthermore, by altering compositions of liposomes, we can regulate the extent of drug incorporation with chylomicrons. Long-chain and unsaturated fatty acids enhance lymphatic transport via chylomicrons. DOPC (18:1 PC) liposome induced to produce large amounts of chylomicron production and helped model drug (BODIPY 505/515) to bind with those chylomicrons.