Development of Tc-99m-5-fluorouracil as a potential tumor diagnostic agent

作者：Dar Ume Kalsoom; Khan Irfan Ullah^*; Javed Muhammad; Ali Muhammad; Hyder Syed Waqar; Murad Sohail; Anwar Jamil

来源：Pakistan Journal of Pharmaceutical Sciences, 2013, 26(2): 333-337.

• 5-Fluorouracil
• radiolabeling
• biodistribution
• tumor
• diagnosis

5-Fluorouracil is a well know drug for chemotherapy of various types of cancer. In the present study, we radiolabeled 5-fluorouracil with Tc-99m for a diagnostic study of cancer. After successful labeling of the drug we performed an animal study to evaluate the potential of this radiopharmaceutical as a tumor diagnostic agent. The results showed 98.1 +/- 1.2 % labeling efficacy of 5-fluorouracil with Tc-99m. The in vitro stability of the radiolabeled drug at room temperature at 4 hr of post-labeling was >96.5 +/- 0.4 %. The binding of the radiolabeled drug with plasma proteins was 66.6 +/- 3%. Partition coefficient results showed that this drug is hydrophilic in nature. Biodistribution study in rabbit models displayed faint uptake in liver. Both kidney and bladder were prominent as excretory route of the labeled drug. Bioevaluation was performed in Swiss Webster mice having naturally developed tumor. Mice were dissected, uptake of drug in various organs was studied and results showed prominent uptake in liver and tumor. Tumor was further investigated by histopathological study.

• 出版日期2013-3