^(153)Sm-聚氨基葡糖的标记及其在小鼠体内的分布  

Preparation of ^(153)Sm-Chitosan complex and its biodistribution in mice

作　　者：周云[1] 刘璐[1] 高文[1] 孙晋[1] 黄鹰[1] 

机构地区：[1]东南大学临床医学院核医学技术研究所,南京210009

出　　处：《中华实验外科杂志》2007年第12期1584-1586,共3页Chinese Journal of Experimental Surgery

基　　金：国家自然科学基金(30470500);江苏省科技厅社会发展资助项目(BS2004020)

摘　　要：目的建立^(153)Sm 标记聚氨基葡糖的方法,观察其通过尾静脉及肝间质内注射给药后在小鼠体内的生物分布,为进一步用于肿瘤治疗奠定基础。方法将^(153)Sm_2O_3与盐酸在适当的条件下制备成^(153)SmCl_3,然后与聚氨基葡糖螯合生成^(153)Sm-CHICO(^(153)Sm-聚氨基葡糖复合物)。昆明种小鼠90只随机分为3组。1、2组小鼠分别经肝间质注射等活度的^(153)Sm-CHICO 和^(153)SmCl_3,3组小鼠经尾静脉注射^(153)Sm-CHICO,剂量为6.1 MBq/0.05 ml,分别于给药后0.5、1、2、6、24及48 h 各组处死5只,取血及主要脏器测定放射性计数率值,计算每克组织的百分注射剂量率(%ID/g),每组各时间点取1只小鼠行 SPECT 显像。结果^(153)Sm-CHICO 的标记率为(95.6±2.7)%,48 h 放化纯为(89.6±1.9)%。1组小鼠肝间质注射^(153)Sm-CHICO 放射性核素主要浓聚于穿刺点,仅有少量分布于注射点外肝脏、肾脏、脾脏、骨等组织器官。1组小鼠肝间质注射点区(直径5 mm)在48 h 百分注射剂量率均值为27.16%ID/g,为2组注射点的139倍,为3组肝组织百分注射剂量率值的131倍。2组和3组小鼠血2 h 的放射性活度为1组130倍以上,且血中放射性计数在较短时间内快速下降。结论^(153)Sm-CHICO 标记方法简单、可行,具有较高的标记率及较好的稳定性。肝间质注射的^(153)Sm-CHICO 较长时间滞留在注射部位局部较小范围,在注射点以外组织和器官分布较少,血液清除快,^(153)Sm-CHICO 可能成为肿瘤核素内照射治疗的一种新药。Objective To establish a method for labeling chitosan with samarium-153 and examine the biodistribution in mice after intrahepatic or intravenous administration of the samarium-153 chitosan complex or samarium-153 chloride solution. Methods Samarium-153 chloride solution was prepared by ^153Sm2O3 and the hydrochloric acid under the suitable condition, and the samarium-153 chitosan complex was prepared by simply mixing acidic solutions of chitosan and samarium-153 chloride solution. 90 Kun- ming mice were randomly divided into 3 groups. The mice in group 1 and group 2 were respectively subjected to the intrahepatic administration of the same dosage of samarium-153 chitosan complex and samarium- 153 chloride solution （6.1 MBq,0.05 ml）, and those in group 3 were administered with samarium-153 chitosan complex through caudal veins. SPECT scanning was carried out before those mice were killed and the blood and major organs and tissues were dissected and weighted at 0. 5 ,1,2,4,24 and 48 h after administration, and the radioactivity of those organs and tissues was measured. Results The labeling efficiency of samarium-153 chitosan complex was （95.6 ±2.7）% and satisfactory in vitro stability was found in the study. The radioactivity in the administration site was 27.16% ID/g within 48 h after administration in group 1 ,which was 139 times higher than that in group 2 and 131 times higher than that in the liver in group 3 respectively. Most of the radioactivity administered was retained in the administration site of the liver lobe in group 1 within 48 h after administration ,and low level of radioactivity in the liver adjacent to the administration site and in the kidneys, spleens and bones. Radioactive concentrations in blood in groups 2 and 3 were 130 times higher than that in group 1 within 2 h after administration,and the radioactive concentration in blood was quickly reduced during a short time and remained at a low level up to 48 h in groups 2 and 3. Conclusion This method of labeling chitosan with samarium-

关 键 词：钐153 放射治疗 生物学 分布 

分 类 号：R73-36[医药卫生—肿瘤]