Interventional Radionuclide Therapy of Hepatocellular Carcinoma: Assessment of Intratumoral Retention of HPMA Copolymers

doi:10.1007/s40242-013-2089-8

Chemical Research in Chinese Universities ›› 2013, Vol. 29 ›› Issue (1): 183-188.doi: 10.1007/s40242-013-2089-8

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Interventional Radionuclide Therapy of Hepatocellular Carcinoma: Assessment of Intratumoral Retention of HPMA Copolymers

YUAN Jian-chao¹, MIAO Cheng-ping¹, ZENG Xian-wu², GUO Hong-yun², WANG Xiao-qi², LIAO Shi-qi², XIE Xiao-li¹

1. Key Laboratory of Eco-environment-related Polymer Materials, Ministry of Education, Key Laboratory of Polymer Materials of Gansu Province, College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou 730070, P. R. China;
2. Department of Nuclear Medicine, Gansu Academy of Medical Sciences & Gansu Provincial Tumor Hospital, Lanzhou 730050, P. R. China

Received:2012-03-05 Revised:2012-07-31 Online:2013-02-01 Published:2013-01-23
Supported by:
Supported by the National Natural Science Foundation of China(No.20964003).

Abstract

Abstract:

To develop new radiopharmaceuticals for the interventional radionuclide therapy of recurrent hepatocellular carcinoma, poly(HPMA)-APMA-DTPA[HPMA=N-(2-hydroxypropyl) methacrylamide; APMA=N-(3-aminopro-pyl)methacrylamide; DTPA=diethylenetriaminepentaacetic acid] was synthesized by free radical precipitation polymerization in acetone/dimethylsulfoxide with N,N′-azobis(isobutyronitrile) as the initiator. The copolymers were characterized with nuclear magnetic resonance(NMR) spectroscopy and gel permeation chromatography(GPC, M_n=2.2×10⁴, M_w/M_n=1.38). Subsequently, poly(HPMA)-APMA-DTPA was conjugated with ^99mTc radionuclide. Prolonged retention of poly(HPMA)-APMA-DTPA conjugate within the tumor tissues was demonstrated by single-photon emission computed tomography computed tomography(SPECT-CT) at 1, 2, 4 and 24 h following intra-tumoral injection of the conjugate to hepatocellular carcinoma xenografts in mice. DTPA-^99mTc was also synthesized and characterized for comparison. The data suggest that the poly(HPMA)-APMA-DTPA conjugates might be useful for the interventional radionuclide therapy of recurrent hepatocellular carcinoma in humans.

Key words: Hepatocellular carcinoma, Interventional radionuclide therapy, HPMA copolymer, Radiotracer

YUAN Jian-chao, MIAO Cheng-ping, ZENG Xian-wu, GUO Hong-yun, WANG Xiao-qi, LIAO Shi-qi, XIE Xiao-li. Interventional Radionuclide Therapy of Hepatocellular Carcinoma: Assessment of Intratumoral Retention of HPMA Copolymers[J]. Chemical Research in Chinese Universities, 2013, 29(1): 183-188.

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Interventional Radionuclide Therapy of Hepatocellular Carcinoma: Assessment of Intratumoral Retention of HPMA Copolymers

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