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

• Published in: Chemical research in Chinese universities Vol. 29; no. 1; pp. 183 - 188
• Main Authors: Yuan, Jian-chao, Miao, Cheng-ping, Zeng, Xian-wu, Guo, Hong-yun, Wang, Xiao-qi, Liao, Shi-qi, Xie, Xiao-li
• Format: Journal Article
• Language: English
• Published: Heidelberg Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01.02.2013; 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%Department of Nuclear Medicine, Gansu Academy of Medical Sciences & Gansu Provincial Tumor Hospital, Lanzhou 730050, P.R.China
• Subjects: Analytical Chemistry; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; HPMA; Inorganic Chemistry; Organic Chemistry; Physical Chemistry; 共聚物; 原发性肝癌; 放射性核素; 治疗; 甲基丙烯酰胺; 计算机断层扫描; 评估; Hepatocellular carcinoma; Interventional radionuclide therapy; Radiotracer; HPMA copolymer
• ISSN: 1005-9040; 2210-3171
• DOI: 10.1007/s40242-013-2089-8

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-aminopropyl）methacrylamide; DTPA=diethylenetriaminepentaacetic acidl 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, Mn=2.2xl04, Mw/Mn=l.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.