Production and biological studies of 111In-bleomycin for diagnosis/ therapy purposes

Fe mycin (Bleomycin) is an anti- neoplastic agent which is used in the treatment of squamous cell carcinoma, Hodgkin's lymphoma, and testicles carcinoma. Due to the progress in application and production of SPECT radioisotopes in nuclear medicine, bleomycin was labeled with In-111 which was well accepted in clinics, In mid 70' s un stability of 111 In-Bleomycin made scientists to ignore this agent as an imaging tool, but in 1984 a new stable complex was prepared and used in clinics. In order to obtain the best labeling reaction conditions, the complex formation was optimized for P H, temperature, time,and amount of bleomycin using I TLC and R TLC methods. The labeled compound was injected to normal rats (weighing 150-200 g). Autopsy on the rats at various time intervals after injection and the data was obtained and compared with In111 chloride in normal rats. The radio- labeling method, utilizes no chromatographic purification of desired compound, due to exact optimization of reaction conditions.Total labeling and formulation of 111In-Bleomycin took about 30 Min, with a yield of 99.8%. 111In-Bleomycin was examined by various chromatographic system and shown to have a consistent final specific activity in excess of 1.39 Ci/m mole (limit of detection). The radio-labeled complex was stable m aqueous solutions at leas for 24 hours species followed by filtration through a 0.22 u filter