A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting

Pu Zhang MS; Zhide Guo MS; Deliang Zhang MS; Chang Liu MS; Guibing Chen MM; Rongqiang Zhuang PhD; Manli Song MS; Hua Wu PhD; Xianzhong Zhang PhD

doi:10.1177/1536012116667327

Molecular Imaging (Sep 2016)

A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting

Pu Zhang MS,
Zhide Guo MS,
Deliang Zhang MS,
Chang Liu MS,
Guibing Chen MM,
Rongqiang Zhuang PhD,
Manli Song MS,
Hua Wu PhD,
Xianzhong Zhang PhD

Affiliations

Pu Zhang MS: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China
Zhide Guo MS: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China
Deliang Zhang MS: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China
Chang Liu MS: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China
Guibing Chen MM: Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, Xiamen, China
Rongqiang Zhuang PhD: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China
Manli Song MS: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China
Hua Wu PhD: Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, Xiamen, China
Xianzhong Zhang PhD: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China

DOI: https://doi.org/10.1177/1536012116667327
Journal volume & issue: Vol. 15

Abstract

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The aim of this study is to develop a copolymer-based single-photon emission computed tomography/magnetic resonance (SPECT/MR) dual-modality imaging agent that can be labeled with both technetium-99m ( 99m Tc) and gadolinium (Gd) and target asialoglycoprotein receptor (ASGPR) via galactose. Monomers of N - p -vinylbenzyl-6-(2-(4-dimethylamino)benzaldehydehydrazono) nicotinate (VNI) for labeling of 99m Tc, 5,8- bis (carboxymethyl)-3-oxo-11-(2-oxo-2-((4-vinylbenzyl)amino)ethyl)-1-(4-vinylphenzyl)-2,5,8,11-tetraazatridecan-13-oic acid (V 2 DTPA) for labeling of Gd, and vinylbenzyl- O -β- d -galactopyranosyl- d -gluconamide (VLA) for targeting ASGPR were synthesized, respectively. Then the copolymer P(VLA-co-VNI-co-V 2 DTPA) ( p VLND 2 ) was synthesized and characterized by gel permeation chromatography, dynamic light scattering, and high-performance liquid chromatography analysis. After labeling with 99m Tc and Gd simultaneously, the radiochemical purity, toxicity, relaxivity (r 1 ), and in vivo SPECT/MR imaging in mice were evaluated. Single-photon emission computed tomography/magnetic resonance imaging and biodistribution results showed that p VLND 2 could target ASGPR well. The significantly improved signal to noise ratio was observed in mice liver during MR imaging. All the results suggest that this novel kind of copolymer has the potential to be further developed as a functional SPECT/MR imaging agent.

Published in Molecular Imaging

ISSN: 1536-0121 (Online)
Publisher: SAGE Publications
Country of publisher: United States
LCC subjects: Science: Biology (General); Medicine: Medicine (General): Medical technology
Website: https://journals.sagepub.com/home/MIX

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