Influence of route of administration and lipidation of apolipoprotein A-I peptide on pharmacokinetics and cholesterol mobilization.

ABSTRACT: apoA-I, apoA-I mimetic peptides, and their lipid complexes or reconstituted high-density lipoprotein (HDL) have been studied as treatments for various pathologies. However, consensus is lacking about the best method for administration, by intravenous (IV) or intraperitoneal (IP) routes, and formulation, as an HDL particle or in a lipid-free form. The objective of this study was to systematically examine peptide plasma levels, cholesterol mobilization, and lipoprotein remodeling in vivo following administration of lipid-free apoA-I peptide (22A) or phospholipid reconstituted 22A-sHDL by IV and IP routes. The mean circulation half-life was longer for 22A-sHDL (T_1/2 = 6.27 h) than for free 22A (T_1/2 = 3.81 h). The percentage of 22A absorbed by the vascular compartment af

SUBMITTER: Tang J 

PROVIDER: S-EPMC5234715 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature