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

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...

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Main Authors: 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
Format: Article
Language:English
Published: SAGE Publications 2016-09-01
Series:Molecular Imaging
Online Access:https://doi.org/10.1177/1536012116667327
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author 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
author_facet 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
author_sort Pu Zhang MS
collection DOAJ
description 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.
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spelling doaj.art-ef2b80cd02d740e29629f4eaf6bbd0132024-03-02T10:53:46ZengSAGE PublicationsMolecular Imaging1536-01212016-09-011510.1177/153601211666732710.1177_1536012116667327A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor TargetingPu Zhang MS0Zhide Guo MS1Deliang Zhang MS2Chang Liu MS3Guibing Chen MM4Rongqiang Zhuang PhD5Manli Song MS6Hua Wu PhD7Xianzhong Zhang PhD8 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, Xiamen, China Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, China Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, Xiamen, China Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, ChinaThe 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.https://doi.org/10.1177/1536012116667327
spellingShingle 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
A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
Molecular Imaging
title A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
title_full A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
title_fullStr A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
title_full_unstemmed A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
title_short A Novel Copolymer-Based Functional SPECT/MR Imaging Agent for Asialoglycoprotein Receptor Targeting
title_sort novel copolymer based functional spect mr imaging agent for asialoglycoprotein receptor targeting
url https://doi.org/10.1177/1536012116667327
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