Metabolic comparison of radiolabeled bleomycin and bleomycin-glucuronide labeled with 99mTc

PubMed ID: 21950554The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with 99mTc ( 99mTc-BLM and 99mTc-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 99mTc, 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 99mTc-BLM and 99mTc-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for 99mTc-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for 99mTc-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 99mTc-BLMG was found to be better than that of 99mTc-BLM. © 2011, Mary Ann Liebert, Inc