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To develop new tumor targeting macromolecular conjugates,poly(HPMA)-SD-APMA-DTPA (HPMA:N-(2-hydroxypropyl)-methacrylamide; APMA:N-(3-aminopropyl)methacrylamide; DTPA:diethylenetriarninepentaacetic acid; SD:sulfadiazine) was synthesized and characterized.The poly(HPMA)-SD-DTPA conjugates were radiolabeled with the radionuclide 99mTc and tested for uptake by cultured H22 cells in vitro.DTPA-99mTc (radiotracer 1) and poly(HPMA)-DTPA-99mTc (radiotracer 2) were also synthesized and characterized for comparison.The uptake of poly(HPMA)-SD-DTPA-99mTc (radiotracer 3,34.76％) was significantly higher than that of poly(HPMA)-DTPA-99mTc (16.40％),indicating that uptake of the poly(HPMA)-SD-DTPA-99mT was active binding.The uptake of poly(HPMA)-DTPA-99mTc was significantly higher than that of DTPA-99mTc (2.98％),suggesting that uptake of the poly(HPMA)-DTPA-99mT was passive binding.The data suggest thin the poly(HPMA)-SD-APMA-DTPA conjugates might be useful as tumor targeting macromolecular conjugates.