南方医科大学学报

南方医科大学学报 ›› 2006, Vol. 26 ›› Issue (03): 361-.

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131I-Herceptin的制备、质控及在新西兰兔的生物分布

范义湘； 罗荣城； 方永鑫； 严晓；   

  1. 南方医科大学南方医院肿瘤中心； 南方医科大学南方医院肿瘤中心 广东广州510515； 广东广州510515；
  • 出版日期:2006-03-20 发布日期:2006-03-20

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

FAN Yi-xiang,LUO Rong-Cheng,FANG Yong-Xin,YAN Xiao,Department of Oncology,Nanfang Hospital,Southern Medical University,Guangzhou 510515,China   

  1. 南方医科大学南方医院肿瘤中心； 南方医科大学南方医院肿瘤中心 广东广州510515； 广东广州510515；
  • Online:2006-03-20 Published:2006-03-20

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摘要： 目的探讨131I-Herceptin的免疫活性、生物分布及代谢规律,为乳腺癌的131I-Herceptin放射免疫治疗提供实验依据。方法①采用Iodogen法对Herceptin进行131I标记,以HPLC法测定放射化学纯度(RCP)。以与BT-474细胞结合率(BR)鉴定131I-Herceptin的免疫活性。②按74 MBq/kg.b.w.对3只新西兰兔注射131I-Herceptin,注射后3 h及第1、3、5天进行透射CT显像。以肌肉为参照,计算各脏器放射性计数比值(O/M)。③第5天处死动物,取血、心、肺、肝、肾等脏器,计算每克组织摄取分数(ID%/g),对结果进行统计分析。结果131I-Herceptin的标记率为93%,RCP为95%,在BT-474细胞结合率为(36.9±4.7)%。注射131I-Herceptin后不同时间均以心脏、肺、肝浓聚显著,肌肉、肠影像稀疏。随时间延迟,心影逐渐稀疏,肝脏影像浓聚。注射后3 h,心脏O/M值显著高于肺及肝、肾、肠等脏器。随时间延迟,心脏O/M值于注射后1 d显著降低(t=10.817,P<0.001),第3、5天亦显著降低,肝脏O/M值在第1、3、5天均比注射后3 h显著下降。每克组织的摄取分数以血液最高,为(11.3 ID/g)%、肝为(2.8 ID/g)%、心肌仅为(1.8 ID/g)%。结论131I-Herceptin的免疫活性高。机体分布以血液、肝、肾为主,心肌摄取量低。

Abstract: Objective To study the immunoactivity,biodistribution and metasbolic pattern of 131I-Herceptin in rabbits.Methods Herceptin was radiolabelled with 131I 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 131I-Herceptin.131I-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 γ-counter to calculate the uptake percentage per gram tissue(ID%/g).Results The labeling rate of 131I-herceptin was 93% with RCP of 95% and binding rate to BT-474 cells of 36.9%.After injection of 131I-herceptin,the heart,lung and liver displayed dense radioactive regions but not the muscles and intestines.Three hours after injection,the O/M ratio of the heart was significantly higher than that of the lung,kidney and intestine(P<0.05),but decreased significantly one day after injection(t=10.817,P<0.001) with further decrement on days 3 and 5(P<0.05).The O/M ratio of liver on day 1,3,and 5 reduced significantly in comparison with that at 3 h(P<0.05).The uptake percentage was higher in the blood(11.3 ID/g%) than in the liver(2.8 ID/g%) and the myocardium(1.8 ID/g%).Conclusions 131I-herceptin possesses high immunoactivity which distributes mainly in the blood,liver and kidney,but with low uptake in the myocardium.

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