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Tumor targeting of HPMA copolymer conjugates containing sulfadiazine groups 被引量:1

Tumor targeting of HPMA copolymer conjugates containing sulfadiazine groups
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摘要 To develop new tumor targeting macromolecular conjugates,poly(HPMA)-SD-APMA-DTPA(HPMA:N-(2-hydroxypropyl)- methacrylamide;APMA:N-(3-ammopropyl)methacrylamide;DTPA:diethylenetriaminepentaacetic acid;SD:sulfadiazine) was synthesized and characterized.The poly(HPMA)-SD-DTPA conjugates were radiolabeled with the radionuclide ^(99m)Tc and tested for uptake by cultured H22 cells in vitro.DTPA-^(99m)Tc(radiotracer 1) and poly(HPMA)-DTPA-^(99m)Tc(radiotracer 2) were also synthesized and characterized for comparison.The uptake of poly(HPMA)-SD-DTPA-^(99m)Tc(radiotracer 3,34.76%) was significantly higher than that of poly(HPMA)-DTPA-^(99m)Tc(16.40%),indicating that uptake of the poly(HPMA)-SD-DTPA-^(99m)T was active binding.The uptake of poly(HPMA)-DTPA-^(99m)Tc was significantly higher than that of DTPA-^(99m)Tc(2.98%), suggesting that uptake of the poly(HPMA)-DTPA-^(99m)T was passive binding.The data suggest that the poly(HPMA)-SDAPMA -DTPA conjugates might be useful as tumor targeting macromolecular conjugates. To develop new tumor targeting macromolecular conjugates,poly(HPMA)-SD-APMA-DTPA(HPMA:N-(2-hydroxypropyl)- methacrylamide;APMA:N-(3-ammopropyl)methacrylamide;DTPA:diethylenetriaminepentaacetic acid;SD:sulfadiazine) was synthesized and characterized.The poly(HPMA)-SD-DTPA conjugates were radiolabeled with the radionuclide ^(99m)Tc and tested for uptake by cultured H22 cells in vitro.DTPA-^(99m)Tc(radiotracer 1) and poly(HPMA)-DTPA-^(99m)Tc(radiotracer 2) were also synthesized and characterized for comparison.The uptake of poly(HPMA)-SD-DTPA-^(99m)Tc(radiotracer 3,34.76%) was significantly higher than that of poly(HPMA)-DTPA-^(99m)Tc(16.40%),indicating that uptake of the poly(HPMA)-SD-DTPA-^(99m)T was active binding.The uptake of poly(HPMA)-DTPA-^(99m)Tc was significantly higher than that of DTPA-^(99m)Tc(2.98%), suggesting that uptake of the poly(HPMA)-DTPA-^(99m)T was passive binding.The data suggest that the poly(HPMA)-SDAPMA -DTPA conjugates might be useful as tumor targeting macromolecular conjugates.
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2012年第7期875-878,共4页 中国化学快报(英文版)
基金 the National Natural Science Foundation of China(No.20964003)for funding
关键词 Tumor targeting HepatoceUular carcinoma HPMA copolymer conjugates Radiotracer Tumor targeting HepatoceUular carcinoma HPMA copolymer conjugates Radiotracer
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