Abstract
Intestinal lymphatic drug delivery has been widely studied because drugs can bypass the first-pass metabolism in the liver via the lymphatic route, which increases oral bioavailability. Various lipid-based nanoparticles have been used to deliver hydrophobic drugs to the lymphatic pathway. This review focuses on the liposomal delivery systems used for intestinal lymphatic drug transport. Liposomal formulations have attracted particular attention because they can stimulate the production of chylomicrons and the incorporated drugs readily associate with enterocyte-derived chylomicrons, enhancing lymphatic drug transport. We believe that a full understanding of their contribution to intestinal drug translocation will lead to effective oral delivery with liposomal formulations.
Highlights
There are many ways to deliver drugs into the body, including oral, pulmonary, subcutaneous, intravenous, transdermal, and nasal
These findings demonstrate that liposomal formulations can play an important role in improving drug stability and bioavailability for oral delivery, by facilitating lymphatic drug transport
During intestinal lymphatic drug transport, long-chain and unsaturated lipids are assembled into chylomicrons in enterocytes
Summary
There are many ways to deliver drugs into the body, including oral, pulmonary, subcutaneous, intravenous, transdermal, and nasal. The drugs pass through the small intestine and enter the portal vein or intestinal lymphatic system (Fig. 1). Some monoglycerides and fatty acids diffuse into enterocytes and enter the portal vein, while others are resynthesized to chylomicrons and secreted into lymphatic vessels. Lipoproteins associated with lipophilic drugs enter intestinal lymphatic vessels and are transported to systemic circulation. Coadministration with lipids can increase the level of drug transport through the intestinal lymphatic system (Fig. 3); Fig. 2 Pathways of lipid absorption and chylomicron synthesis within enterocytes. Lipid-conjugated drugs Drugs modified with a lipid moiety, such as a fatty acid, glyceride, or phospholipid, show increased lipophilicity (Fig. 4). These lipid-conjugated drugs can be associated into enterocyte-derived chylomicrons. Gert Fricker et al used a phospholipid–valproic acid conjugate as a model drug for oral delivery [13]
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