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Reconstituted high-density lipoprotein (rHDL) is a synthetic or biomimetic nanoparticle designed to closely mimic the structure and function of endogenous human high-density lipoprotein (HDL). rHDL is typically composed of apolipoprotein A-I (apoA-I) combined with phospholipids, forming discoidal particles that resemble native HDL in both chemical composition and biological activity. The primary mechanism of action involves facilitating reverse cholesterol transport by promoting cholesterol efflux from peripheral tissues—especially macrophages in atherosclerotic plaques—via interaction with cellular receptors such as scavenger receptor class B type 1 (SR-B1) and ATP-binding cassette transporters ABCA1 and ABCG1. In addition to its natural role in lipid metabolism, rHDL has been developed as a drug delivery platform for targeted therapy, particularly for cardiovascular diseases like atherosclerosis and for tumor-targeted delivery of anti-cancer agents. As a drug carrier, rHDL can encapsulate hydrophobic or amphiphilic drugs, improving their bioavailability while reducing off-target toxicity. Clinical studies have evaluated rHDL infusions for rapid reduction of coronary plaque burden after acute coronary syndromes; results suggest potential vascular benefits but further large-scale trials are needed[3][4][6][8].
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