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目的研究188Re-奥曲肽在荷瘤裸鼠体内的分布,为进一步肿瘤靶向治疗奠定基础。方法16只荷人H460非小细胞肺癌的BALB／c裸鼠分为4组,经尾静脉注射188Re-奥曲肽 18．5MBq(O．2ml)．于注射后2h,4h,24h,48h每个时间点处死一组裸鼠,取血液、肿瘤组织及主要脏器测量其放射性计数率值,经放射性衰变校正后计算每克组织的百分注射剂量率(％ID／g),观察标记物在动物体内的生物学分布。另2只荷瘤裸鼠同样尾静脉注射相同剂量的188Re-奥曲肽,于注射后相同时间点行SPECT扫描,利用感兴趣区技术对肿瘤／非瘤组织放射性比值(T／NT)进行半定量分析。结果188Re-奥曲肽标记率达(95．3±1．8)％,188Re-奥曲肽在荷瘤裸鼠体内主要分布于肿瘤组织、肝脏、肾脏及肠道,肿瘤部位在4h摄取达到高峰9．8％ID/g,此时SPECT在肿瘤部位有明显的放射性核素浓聚,T／NT在尾静脉药物注射后24h达到高值为7．1。结论 188Re-奥曲肽在BALB／c荷瘤裸鼠体内对人非小细胞肺癌具有靶向定位作用,其在肿瘤部位的分布具有较高的T／NT,188Re．奥曲肽有望用于表达生长抑素受体肿瘤的核素靶向治疗。
Objective To study the distribution of 188Re-octreotide in tumor-bearing nude mice and lay the foundation for further tumor targeting therapy. Methods Twenty-six BALB / c nude mice bearing human H460 non-small cell lung cancer were divided into 4 groups, and 188Re-octreotide 18.5MBq (O.2ml) was injected through tail vein. A group of nude mice were sacrificed at 2h, 4h, 24h and 48h after injection respectively. The radioactive count rate was measured by blood, tumor tissues and major organs. After radioactive decay, the percentage of injected dose per gram of tissue was calculated Rate (% ID / g), observe the biological distribution of the marker in the animal body. The other two tumor-bearing nude mice also received the same dose of 188Re-octreotide at the same tail vein. SPECT scans were performed at the same time point after injection. Semi-quantitative analysis of tumor / non-tumor tissue radioactivity ratio (T / NT) . Results 188Re-octreotide labeling rate (95.3 ± 1.8)%, 188Re-octreotide in tumor-bearing nude mice mainly in tumor tissue, liver, kidney and intestine, the tumor site uptake at 4h 9.8 % ID / g. At this time, SPECT had obvious radionuclide accumulation in the tumor site, and T / NT reached a high value of 7.1 after 24h of tail vein injection. Conclusion 188Re-octreotide targets in human non-small cell lung cancer in BALB / c tumor-bearing nude mice and has a high T / NT and 188Re distribution in tumor sites. Octreotide is expected to be used to target radionuclide targeting somatostatin receptor tumors.