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. Author manuscript; available in PMC: 2018 Jun 1.
Published in final edited form as: Biomaterials. 2017 Mar 26;130:1–13. doi: 10.1016/j.biomaterials.2017.03.024

Scheme 1. Design of a hepatocyte-specific anti-atherogenic gene delivery system.

Scheme 1

Cholesterol (>80 % in the form of cholesteryl esters (CE)) is transported by HDL from atherosclerotic plaque-associated macrophage foam cells to the liver by the process of reverse cholesterol transport (RCT), subsequently converted to bile acids (BA), and eliminated from bile/feces. Galactose-functionalized PAMAM dendrimer G5, i.e., Gal-G5, is developed as a hepatocyte-specific gene delivery system to deliver CEH expression vector. Galactose facilitates ASGPR-mediated endocytosis of Gal-G5/CEH complexes into hepatocytes in the liver and increases CEH expression. The overexpressed CEH would enhance the hydrolysis of HDL-CE into free cholesterol (FC), which is either directly secreted into bile or converted to bile acids followed by elimination from the body - a process proposed to regress the existing atherosclerotic plaques.