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Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging.

Abstract：

:Galactosylated chitosan (GC) was prepared by reacting lactobionic acid with water-soluble chitosan. GC was labeled with fluorine-18 by conjugation with N-succinimidyl-4-(18)F-fluorobenzoate ([(18)F]SFB) under a slightly basic condition. After rapid purification with HiTrap desalting column, [(18)F]FB-GC was obtained with high radiochemical purity (>97%) determined by radio-HPLC. The total reaction time for [(18)F]FB-GC was about 150 min. Typical decay-corrected radiochemical yield was about 4-8%. Ex vivo biodistribution in normal mice showed that [(18)F]FB-GC had moderate activity accumulation in liver with very good retention (11.13+/-1.63, 10.97+/-1.90 and 10.77+/-0.95%ID/g at 10, 60, 120 min after injection, respectively). The other tissues except kidney showed relative low radioactivity accumulation. The high liver/background ratio affords promising biological properties to get clear images. The specific binding of this radiotracer to the ASGP receptor was confirmed by blocking experiment in mice. Compared with the non-blocking group the hepatic uptake of [(18)F]FB-GC significantly declined in all selected time points. The better liver retention properties of [(18)F]FB-GC than that of albumin based imaging agents may improve imaging quality and simplify pharmacokinetic model of liver function in the future application with PET imaging.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yang W,Mou T,Guo W,Jing H,Peng C,Zhang X,Ma Y,Liu B

doi

10.1016/j.bmcl.2010.06.106

subject

Has Abstract

pub_date

2010-08-15 00:00:00

pages

4840-4

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00893-0

journal_volume

20

pub_type

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