Studies on malignant cancer with sup(99m)Tc-labelled bleomycin

Bleomycin (BLM), a group of the basic glycopeptide anti-biotics with antitumor properties that is produced by a strain Streptomyces verticillus, is a chemotherapeutic agent known to concentrate highly in tumor cells. Therefore, the potential value of BLM labelled with sup(99m)Tc as a tumor-seeking agent was studied in tissues of rats and mice bearing a Walker 256 carcinoma and Sarcoma 180 tumor cells. The optimal labelling procedure for BLM with sup(99m)Tc, using Sn(II) as the reductant are; pH value between 7.0 and 8.5 and Sn(II) concentration of 10-5 M. Bleomycin concentration has no influence and the chemical stability of the sup(99m)Tc complex is stable during 3 hours at room temperature. Under these condition, approximately 90% of labelling was investigated by thin layer chromatographic analysis. Various organs distribution were observed after intravenous administration of the sup(99m)-BLM into Walker 256 carcinoma and Sarcoma 180 tumor bearing rats and mice after 1 hr, 3 hrs and 5 hrs.The concentration of Walker 256 carcinoma and Sarcoma 180 tumor by sup(99m)Tc-BLM was 0.2% and 0.5%, respectively, administrated activity after an hour. Tumor uptake of sup(99m)Tc-BLM was concentrate slightly more than all organs except kidney and blood. (Author)