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目的探讨131I-BDI-1在荷人膀胱癌裸鼠模型中的体内生物分布和对肿瘤的靶向定位性能以及其生物安全性,并由此估算131I-BDI-1在人体内主要脏器的内照射吸收剂量和人体有效剂量。方法通过氯胺-T法用131I溶液直接标记抗人膀胱癌单克隆抗体BDI-1,制备131I-BDI-1,荷人膀胱癌EJ细胞裸鼠尾静脉注射222kBq131I-BDI-1后,于不同时刻处死动物,取感兴趣器官和组织,称重并测量放射性计数,计算131I-BDI-1在荷瘤裸鼠中的标准摄取值和靶/非靶组织比值。利用标准的MIRD数据表计算人体的%ID/g,通过MIRDOSE3.1软件估算131I-BDI-1对人体各个器官的辐射吸收剂量及有效剂量。结果生物分布数据示131I-BDI-1血液清除缓慢,肿瘤部位放射性明显持续滞留,除血液外,具有较高的靶/非靶组织比值。131I-BDI-1人体内照射的有效剂量为1.46×10-2mGy/MBq。结论131I-BDI-1对肿瘤有良好的靶向性,有望成为一种新型的针对人膀胱癌肿瘤的诊治药物,其辐射吸收剂量较低,作为肿瘤治疗药物是安全的。
OBJECTIVE: To investigate the biological distribution of 131I-BDI-1 in vivo and its targeting to tumors in nude mice bearing human bladder cancer and its biosafety, and to evaluate the bioavailability of 131I-BDI-1 in human organs Internal radiation absorbed dose and effective dose of human body. Methods 131I-BDI-1 was prepared by direct labeling of anti-human bladder cancer monoclonal antibody BDI-1 with 131I solution by chloramine-T method. After injection of 222kBq131I-BDI-1 into tail vein of human bladder cancer EJ cells, Animals were sacrificed at all times, organs and tissues of interest were taken, radioactivity counts were weighed and measured, and the standard uptake of 131I-BDI-1 in tumor-bearing nude mice and the ratio of target / non-target tissue were calculated. Human body% ID / g was calculated using a standard MIRD data table, and the radiation-absorbed doses and effective doses of 131I-BDI-1 to various organs of the human body were estimated by MIRDOSE 3.1 software. Results The biodistribution data showed that 131I-BDI-1 had a slow blood clearance and persistent radioactivity at the tumor site. In addition to blood, it had high target / non-target tissue ratio. The effective dose of 131I-BDI-1 for human body irradiation is 1.46 × 10 -2 mGy / MBq. Conclusion 131I-BDI-1 has a good targeting on tumor and is expected to become a new diagnostic and therapeutic agent for human bladder cancer with low radiation absorbed dose and safe as a tumor therapeutic agent.