Metabolic Comparison of Radiolabeled Bleomycin and Bleomycin-Glucuronide Labeled with Tc-99m

Kocan F., Avcibasi U., ÜNAK P. , Muftuler F. Z. B. , İÇHEDEF Ç. , Demiroglu H., ...More

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, vol.26, no.5, pp.573-584, 2011 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 5
  • Publication Date: 2011
  • Doi Number: 10.1089/cbr.2011.0998
  • Page Numbers: pp.573-584


The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with Tc-99m (Tc-99m-BLM and Tc-99m-BLMG, respectively) has been investigated in this study. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. To compare the metabolic behavior of BLM and its glucuronide conjugate radiolabeled with Tc-99m, scintigraphic, and biodistributional techniques were applied using male New Zealand rabbits and Albino Wistar rats. The results obtained have shown that these compounds were successfully radiolabeled with a labeling yield of about 100%. Maximum uptakes of Tc-99m-BLM and Tc-99m-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for Tc-99m-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for Tc-99m-BLMG, respectively. Scintigraphy and biodistributional studies performed on the experimental animals have shown that radiopharmaceutical potentials of these compounds are completely different. At the same time, uptake of the Tc-99m-BLMG was found to be better than that of Tc-99m-BLM.