PET/MRI双模态显像剂^(68)Ga-NOTA-SPIO的制备及其性质初步研究  

Preparation and Properties of ^(68)Ga-NOTA-SPIO as PET/MRI Dual-modal Imaging Agent

作　　者：吴凡[1,2] 王欣璐[2] 尹吉林[1,2] 张金赫[2] 欧阳习[2] 周崝[2] 杨玉婷[2] 钟建秋[2] 

机构地区：[1]南方医科大学,广东广州510515 [2]广州军区广州总医院核医学科,广东广州510010

出　　处：《中国医学影像学杂志》2017年第5期329-334,共6页Chinese Journal of Medical Imaging

基　　金：国家自然科学基金(81571733);广东省自然科学基金(2016A030313612);广东省省级科技计划项目(2014A020212261);广州市产学研协同创新重大专项(201604020094);广州市科技计划项目(201510010278)

摘　　要：目的制备高灵敏度、高分辨率的PET/MRI双模态显像探针^(68)Ga-NOTASPIO,对其体外及部分体内生物学性质进行评价,并探讨其作为PET/MRI双模态显像剂的可能。材料与方法制备出前体SPIO-PEG2000-NOTA,并对其表征进行检测。采用"一锅法"对前体进行放射性标记,制备出双模态探针^(68)Ga-NOTA-SPIO,采用快速薄层层析法测定标记率。评估其体外稳定性和脂水分配系数,并观察其在正常鼠的体内生物学分布。结果制备出分散均一、粒径均匀的前体SPIO-PEG2000-NOTA;并合成双模态探针^(68)Ga-NOTA-SPIO,标记率达99%,脂水分配系数Log P=-2.60±0.13,在磷酸盐缓冲液和胎牛血清中2 h内的放化纯度均>95%。小鼠体内生物分布实验显示,该探针主要分布于肝脏和脾脏,血液中廓清速度较快。结论 "一锅法"合成双模态探针^(68)Ga-NOTA-SPIO标记率高、无需纯化,具有良好的理化性质及生物相容性,可用于后续的PET/MRI双模态显像研究。Purpose To prepare ^68Ga-NOTA-SPIO as PET/MRI dual mode imaging probe with high sensitivity and resolution, and further evaluate its in vitro and partly in vivo biological properties. Materials and Methods The precursor SPIO-PEG,^68-NOTA was prepared and characterized. The precursor was radiolabeled by using ＂one step＂ method to prepare^68Ga-NOTA-SPIO as dual mode imaging probe. The labeling rate of the probe was determined by rapid thin-layer chromatography. Besides, the in vitro stability and lipid water partition coefficient of the probe were evaluated, and its biodistribution in normal mice was also observed. Results The precursor SPIO-PEG2000-NOTA with uniform dispersion and unitbrm particle size was prepared, and the dual mode probe ^68Ga-NOTA- SPIO was synthesized. The labeling rate reached 99% and the lipid water partition coefficient （Log P） was （ 2.60±0.13）. The radiochemical purity of the probe was higher than 95%, as it was incubated in the phosphate buffer and fetal bovine serum within 2 hours. The probe was mainly distributed in the liver and spleen of mice, and its clearance velocity in blood was last. Conclusion The double mode probe ^68Ga-NOTA-SPIO synthesized by one step method has high labeling rate with no need of purification, which has good physic-chemical properties and biocompatibility. The probe can be used in the further research of PET/MRI dual modality imaging.

关 键 词：正电子发射断层显像术 磁共振成像 纳米粒子 镓放射性同位素 分子探针 诊断显像 

分 类 号：R33[医药卫生—人体生理学] R445.6[医药卫生—基础医学]