CAJ | 학술논문

目的通过99Tcm一步法对DTPA-DG钆盐(Gd-DTPA-DG)进行标记,并观察标记物的稳定性及在荷瘤裸鼠体内的生物分布.方法首先合成DTPA-DG,再与Gd2O3螯合,制得Gd-DTPADG.采用1.5T超导型MR扫描仪观察Gd-DTPA-DG在荷瘤裸鼠体内的肿瘤靶向效果,用正交实验设计对Gd-DTPA-DG进行99Tcm标记,采用薄层色谱法分析标记率;用SPECT仪观察标记药物在裸鼠体内的分布.裸鼠体内注入标记药物后10,30 min和1,2,4,24 h测定血液、心、脑、肝、脾、肺、肾、小肠、肌肉、肿瘤中的%ID/g.结果 Gd-DTPA-DG在荷瘤裸鼠体内显示出良好的肿瘤靶向效果.99TcmGd-DTPA-DG的放化纯约98.5%;体外放置6 h,放化纯为96.2%.2 h时肿瘤组织显像清晰,肿瘤组织对99Tcm-Gd-DTPA-DG的摄取为(1.48±0.12)%ID/g,肿瘤与肌肉的放射性比值达2.91.结论 MRI示合成的Gd-DTPA-DG可使肿瘤强化;用99Tcm标记Gd-DTPA-DG是可行的,标记物在裸鼠体内显示出良好的肿瘤靶向性,是一种极具发展潜力的SPECT-MRI双功能制剂.
목적 통과99Tcm일보법대DTPA-DG구염(Gd-DTPA-DG)진행표기,병관찰표기물적은정성급재하류라서체내적생물분포.방법 수선합성DTPA-DG,재여Gd2O3오합,제득Gd-DTPADG.채용1.5T초도형MR소묘의관찰Gd-DTPA-DG재하류라서체내적종류파향효과,용정교실험설계대Gd-DTPA-DG진행99Tcm표기,채용박층색보법분석표기솔;용SPECT의관찰표기약물재라서체내적분포.라서체내주입표기약물후10,30 min화1,2,4,24 h측정혈액、심、뇌、간、비、폐、신、소장、기육、종류중적%ID/g.결과 Gd-DTPA-DG재하류라서체내현시출량호적종류파향효과.99TcmGd-DTPA-DG적방화순약98.5%;체외방치6 h,방화순위96.2%.2 h시종류조직현상청석,종류조직대99Tcm-Gd-DTPA-DG적섭취위(1.48±0.12)%ID/g,종류여기육적방사성비치체2.91.결론 MRI시합성적Gd-DTPA-DG가사종류강화;용99Tcm표기Gd-DTPA-DG시가행적,표기물재라서체내현시출량호적종류파향성,시일충겁구발전잠력적SPECT-MRI쌍공능제제.
Objective To evaluate the stability and biodistribution of a novel SPECT-MRI bi-functional agem 99Tcm-Gd-DTPA-DG in tumor-bearing nude mice. Methods DTPA-DG was synthesized and then conjugated with Gd2O3 to generate Gd-DTPA-DG. The tumor-bearing nude mice were scanned by MRI to evaluate the tumor targeting ability of Gd-DTPA-DG. The orthogonal experiment was applied to optimize pH value of reaction medium and reaction temperature. The radiolabeling efficiency was measured by thin layer chromatography. The distribution of 99Tcm-Gd-DTPA-DG in nude mice was evaluated by scintigrapy in vivo. The % ID/g was measured at different time after intravenous injection of 99Tcm-Gd-DTPA-DG. Results The tumor was significantly enhanced by Gd-DTPA-DG with MRI. The radiochemical purity of 99Tcm-Gd-DTPADG was about 98.5% and remained 96.2% at room temperature for 6 h. The tumor was well visualized by 99TcmGd-DTPA-DG SPECT at 2 h after injection. The tumor uptake was (1.48 ±0.12) %ID/g, and the rumor to muscle radioactivity ratio was 2.91. Conclusions MRI contrast of Gd-DTPA-DG may enhance tumor detection. 99Tcm-labeled Gd-DTPA-DG may be useful for tumor imaging and might have a potential role as a SPECT-MRI bi-functional agent.