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Journal of Bioactive and Compatible Polymers
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Tumor-Selective Macromolecular MRI Contrast Agents

Guo-Ping Yan

Ren-Xi Zhuo

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

Yun-Huang Yang

Li-Yun Li

Mai-Li Liu

Chao-Hui Ye

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

Tumor-selective macromolecular ligands containing 5-(p-Carbonyloxyphenyl)-10,15,20-triphenylporphyrin (HPTP) moiety (PHEA-DTPAHPTP and PAEA-DTPA-HPTP) were prepared by the incorporation of diethylenetriaminepentaacetic acid (DTPA) and 5-(p-hydroxylphenyl)-10,15, 20-triphenylporphyrin (HPTP) as the tumor-selective group in poly [{alpha},ß-(N-(2-hydroxyethyl)-L-aspartamide)] (PHEA) and poly-[{alpha}-ß-(N-(2-aminoethy1)-L-aspartamide)] (PAEA). These ligands were further complexed with gadolinium chloride to form two tumor-selective macromolecular MRI contrast agents PHEA-Gd-DTPA-HPTP and PAEA-Gd-DTPA-HPTP. Relaxivity studies showed that both the polyaspartamide-gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of tumors in mice indicated that these two polyaspartamide MRI contrast agents containing 5-(p-Carbonlyoxyphenyl)-10,15,20-triphenylporphyrin moiety can significantly enhance the contrast MRIs of Hepatoma (H22) and Ehrlich ascites carcinoma after injection and are taken up selectively by these cancers in mice.

Journal of Bioactive and Compatible Polymers, Vol. 17, No. 2, 139-151 (2002)
DOI: 10.1106/088391102024234
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G.-P. Yan, S. E. Bottle, R.-X. Zhuo, L. Wei, M.-L. Liu, and L.-Y. Li
Evaluation of Dendritic Gadolinium Complexes as MRI Contrast Agents
Journal of Bioactive and Compatible Polymers, November 1, 2004; 19(6): 453 - 465.
[Abstract] [PDF]