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Liver-targeting macromolecular MRI contrast agents

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Abstract

Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-α, β-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(III) contents. These macromolecular ligands and their gadolinium complexes were characterized by1H NMR, IR, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property.

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Authors and Affiliations

  1. Laboratory of Biomedical Polymer Materials of the Ministry of Education, Department of Chemistry, Wuhan University, 430072, Wuhan, China

    Guoping Yan, Renxi Zhuo & Mianyi Xu

  2. State Key Laboratory of Magnetic Resonance and Atomic and Molecular Physics, Wuhan Institute of Physics and Mathematics, Chinese Academy of Sciences, 430071, Wuhan, China

    Liyun Li & Yuefeng Tang

Authors
  1. Guoping Yan
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  2. Renxi Zhuo
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  3. Mianyi Xu
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  4. Liyun Li
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  5. Yuefeng Tang
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Correspondence to Renxi Zhuo.

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Yan, G., Zhuo, R., Xu, M. et al. Liver-targeting macromolecular MRI contrast agents. Sc. China Ser. B-Chem. 44, 344–352 (2001). https://doi.org/10.1007/BF02879808

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  • DOI: https://doi.org/10.1007/BF02879808

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