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Synthesis and characterization of poly(HPMA)‐APMA‐DTPA‐ 99m Tc for imaging‐guided drug delivery in hepatocellular carcinoma
Author(s) -
Yuan Jianchao,
Miao Chengping,
Peng Fangyu,
Zeng Xianwu,
Guo Hongyun,
Wang Xiaoqi,
Liao Shiqi,
Xie Xiaoli
Publication year - 2012
Publication title -
journal of applied polymer science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.575
H-Index - 166
eISSN - 1097-4628
pISSN - 0021-8995
DOI - 10.1002/app.38065
Subject(s) - hepatocellular carcinoma , in vivo , methacrylamide , cancer research , chemistry , in vitro , biodistribution , microbiology and biotechnology , pathology , medicine , biology , copolymer , biochemistry , acrylamide , organic chemistry , polymer
To develop a theranostic agent for diagnostic imaging and treatment of hepatocellular carcinoma (HCC), poly(HPMA)‐APMA‐DTPA‐ 99m Tc (HPMA: N ‐(2‐hydroxypropyl methacrylamide; APMA: N ‐(3‐aminopropyl)methacrylamide; DTPA: diethylenetriaminepentaacetic acid) and DTPA‐ 99m Tc were synthesized and characterized, and their HCC targeting was tested by in vitro cellular uptake and in vivo tumor imaging in this study. Radioactivity of HCC cells incubated with poly(HPMA)‐APMA‐DTPA‐ 99m Tc was significant higher (16.40%) than that of the cells incubated with DTPA‐ 99m Tc (2.98%). Scintigraphic images of HCC in mice obtained at 8 h after injection of poly(HPMA)‐APMA‐DTPA‐ 99m Tc showed increased radioactivity compared with that in mice injected with DTPA‐ 99m Tc. The results of postmortem tissue radioactivity assay demonstrated higher radioactivity of HCC tumor tissues (2.69 ± 0.15% ID/g) from the tumor‐bearing mice injected with poly(HPMA)‐APMA‐DTPA‐ 99m Tc compared with that of HCC tumor tissues in the tumor‐bearing mice injected with DTPA‐ 99m Tc (0.83 ± 0.03 %ID/g), ( P <0.001). These results first directly confirm the significant passive hepatocellular tumor targeting of HPMA copolymer. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013