Asialoglycoprotein Receptor-Targeted Superparamagnetic Perfluorooctylbromide Nanoparticles.

Background: The decrease in asialoglycoprotein receptor (ASGPR) levels is observed in patients with chronic liver disease and liver tumor. The aim of our study was to develop ASGPR-targeted superparamagnetic perfluorooctylbromide nanoparticles (M-PFONP) and wonder whether this composite agent could target buffalo rat liver (BRL) cells in vitro and could improve R 2 ^∗ value of the rat liver parenchyma after its injection in vivo.
Methods: GalPLL, a ligand of ASGPR, was synthesized by reductive amination. ASGPR-targeted M-PFOBNP was prepared by a film hydration method coupled with sonication. Several analytical methods were used to investigate the characterization and safety of the contrast agent in vitro. The in vivo MR T 2 ^∗ mapping was performed to evaluate the enhancement effect in rat liver.
Results: The optimum concentration of Fe ₃ O ₄ nanoparticles inclusion in GalPLL/M-PFOBNP was about 52.79  µ g/mL, and the mean size was 285.6 ± 4.6 nm. The specificity of GalPLL/M-PFOBNP for ASGPR was confirmed by incubation experiment with fluorescence microscopy. The methyl thiazolyl tetrazolium (MTT) test showed that there was no significant difference in the optical density (OD) of cells incubated with all GalPLL/M-PFOBNP concentrations. Compared with M-PFOBNP, the increase in R 2 ^∗ value of the rat liver parenchyma after GalPLL/M-PFOBNP injection was higher.
Conclusions: GalPLL/M-PFOBNP may potentially serve as a liver-targeted contrast agent for MR receptor imaging.
Competing Interests: The authors declare no conflicts of interest.
(Copyright © 2021 Yang Li et al.)