Preparation, quality control and biodistribution of 131I-herceptin in New Zealand rabbits

• Published in: Nan fang yi ke da xue xue bao = Journal of Southern Medical University Vol. 26; no. 3; p. 361
• Main Authors: Fan, Yi-xiang, Luo, Rong-cheng, Fang, Yong-xin, Yan, Xiao
• Format: Journal Article
• Language: Chinese
• Published: China 01.03.2006
• Subjects: Animals; Antibodies, Monoclonal - administration & dosage; Antibodies, Monoclonal - metabolism; Antibodies, Monoclonal - pharmacokinetics; Antibodies, Monoclonal, Humanized; Antineoplastic Agents - administration & dosage; Antineoplastic Agents - pharmacokinetics; Antineoplastic Agents - standards; Binding, Competitive; Cell Line, Tumor; Chromatography, High Pressure Liquid; Female; Humans; Injections, Intravenous; Iodine Radioisotopes - administration & dosage; Iodine Radioisotopes - metabolism; Iodine Radioisotopes - pharmacokinetics; Male; Quality Control; Rabbits; Time Factors; Tissue Distribution; Trastuzumab
• ISSN: 1673-4254

To study the immunoactivity,biodistribution and metabolic pattern of (131)I-Herceptin in rabbits. Herceptin was radiolabelled with (131)I and its radiochemicalpurity (RCP) measured by size-exclusion high-pressure liquid chromatography (HPLC). The binding rate to BT-474 cells was measured to evaluate the immunoactivity of (131)I-Herceptin. (131)I-herceptin (2.0 mCi/kg) was injected intravenously into New Zealand rabbits. Scintigraphy on emission computed tomography was performed at 3 h, 1, 3 and 5 days after injection, and the radiocounts of the heart, liver and kidney etc. were compared with that of the muscle to calculate the organ-to-muscle activity ratio (O/M). On the fifth day,the rabbits were killed and the blood, myocardium, lung and other organs were obtained for measuring the radiocounts on gamma-counter to calculate the uptake percentage per gram tissue (ID%/g). The labeling rate of (131)I-herceptin was 93% with RCP of 95% and binding rate to BT-474 cells of 36.9%. After injection of (131)I-herceptin