Development of 99mTc-5-fluorouracil as a potential tumor diagnostic agent.

Abstract

5-Fluorouracil is a well know drug for chemotherapy of various types of cancer. In the present study, we radiolabeled 5-fluorouracil with (99m)Tc 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 (99m)Tc. 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.

• Authors: Ume-Kalsoom Dar, Irfanullah Khan, Muhammad Javed, Muhammad Ali, Syed Waqar Hyder, Sohail Murad, Jamil Anwar
• Journal: Pakistan journal of pharmaceutical sciences (Pak J Pharm Sci) Vol. 26 Issue 2 Pg. 333-7 (Mar 2013) ISSN: 1011-601X [Print] Pakistan
• PMID: 23455204 (Publication Type: Evaluation Study, Journal Article)

Chemical References

• Organotechnetium Compounds
• Radiopharmaceuticals
• technetium 99m 5-fluorouracil
• Fluorouracil

Topics

• Animals
• Drug Stability
• Fluorouracil (administration & dosage, analogs & derivatives, pharmacokinetics)
• Hydrophobic and Hydrophilic Interactions
• Isotope Labeling
• Kidney (diagnostic imaging, metabolism)
• Liver (diagnostic imaging, metabolism)
• Male
• Mice
• Organotechnetium Compounds (administration & dosage, pharmacokinetics)
• Protein Binding
• Rabbits
• Radionuclide Imaging
• Radiopharmaceuticals (administration & dosage, pharmacokinetics)
• Sex Cord-Gonadal Stromal Tumors (diagnostic imaging, metabolism, pathology)
• Temperature
• Testicular Neoplasms (diagnostic imaging, metabolism, pathology)
• Tissue Distribution
• Urinary Bladder (diagnostic imaging, metabolism)