Functional evaluation of poly-(N-ρ-vinylbenzyl-O-β-Dgalactopyranosyl-[1-4]-D-gluconamide)(PVLA) as a liver specific carrier

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Abstract
Hepatocytes express the specific C-type lectin, asialoglycoprotein (ASGP) receptor, on the surface to remove the ligand-bearing proteins from circulation. The specific expression and ligand specificity are thought to be the ideal characters for the target of drug or gene delivery. Various galactose-bearing molecules were synthesized for this purpose. However, the biological or functional interaction of these molecules with the ASGP receptor still remains to be elucidated. In this study, we evaluated the functional ability of synthetic galactose polymer ligand, poly-(N-ρ-vinylbenzyl-O-β-Dgalactopyranosyl-[1-4]-D-gluconamide) (PVLA), to interact with recombinant ASGP receptors using mouse ASGP receptor (mouse hepatic lectin; MHL) gene-transfected CHO cells. PVLA-coated beads bound to and were endocytosed by the whole (MHL-1/-2) ASGP receptor-expressing CHO cells like hepatocytes while PVMA (poly-(N-ρ-vinylbenzyl-O-β-D-glucopyranosyl-[1-4]-D-gluconamide) did not. Interestingly, PVLA-coated beads were also en...