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...
Main Authors: | , , , , , , , , |
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Format: | Article |
Language: | English |
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SAGE Publications
2016-09-01
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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. |
first_indexed | 2024-03-07T18:01:11Z |
format | Article |
id | doaj.art-ef2b80cd02d740e29629f4eaf6bbd013 |
institution | Directory Open Access Journal |
issn | 1536-0121 |
language | English |
last_indexed | 2024-03-07T18:01:11Z |
publishDate | 2016-09-01 |
publisher | SAGE Publications |
record_format | Article |
series | Molecular Imaging |
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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