用于血管内放射治疗（IVRT）的潜在（166）钬放射性药物-I：[(166)Ho]钬标记的乙二巯基丁二酸

Potential (166)Ho radiopharmaceuticals for intravascular radiation therapy (IVRT)-I: [(166)Ho] holmium labeled ethylene dicysteine.

作者信息

Chakraborty S, Unni P R, Banerjee S, Samuel G, Das T, Sarma H D, Ramamoorthy N, Pillai M R

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, 400085, Mumbai, India.

出版信息

Nucl Med Biol. 2001 Apr;28(3):309-17. doi: 10.1016/s0969-8051(00)00197-9.

DOI:10.1016/s0969-8051(00)00197-9

PMID:11323243

Abstract

The use of beta(-) emitting radionuclides in the control of restenosis in post angioplasty patients is currently under intense investigation at many leading cardiovascular research centers. (32)P coated metallic stents, (192)Ir wire source and balloons filled with an appropriate radionuclide solution such as of (188)Re, attached to catheter are being studied. (166)Ho has comparable radionuclidic properties to that of (188)Re, can be more easily produced and hence is an attractive alternative to (188)Re. Ethylene dicysteine complex of (166)Ho was prepared and its pharmacological behavior studied. Optimum conditions for the preparation of complex with respect to the reaction time, ligand concentration, pH of the reaction mixture as well as reaction temperature were standardized. The stability of the labeled complex at room temperature as well as at 4 degrees C was determined. Biodistribution pattern of the injected complex in Wistar rats was estimated at 10 min, 30 min and 3 h post injection. This study indicated that >90% of the injected (166)Ho-EC complex was excreted in urine within 3 h post injection, with insignificant retention in any major organ. These studies reveal that (166)Ho-EC could be a viable substitute for (188)Re compounds in radioactive liquid-filled balloon IVRT.

摘要

目前，许多顶尖心血管研究中心正在深入研究使用发射β⁻的放射性核素控制血管成形术后患者的再狭窄情况。正在研究涂有（³²）P的金属支架、（¹⁹²）Ir线源以及连接在导管上并填充有合适放射性核素溶液（如（¹⁸⁸）Re）的球囊。（¹⁶⁶）Ho具有与（¹⁸⁸）Re相当的放射性核素性质，生产起来更容易，因此是（¹⁸⁸）Re的一个有吸引力的替代物。制备了（¹⁶⁶）Ho的乙二巯基络合物并研究了其药理行为。对反应时间、配体浓度、反应混合物的pH值以及反应温度等络合物制备的最佳条件进行了标准化。测定了标记络合物在室温以及4℃下的稳定性。在注射后10分钟、30分钟和3小时估计了注射的络合物在Wistar大鼠体内的生物分布模式。这项研究表明，注射的（¹⁶⁶）Ho-EC络合物在注射后3小时内>90%经尿液排出，在任何主要器官中的滞留量都微不足道。这些研究表明，在放射性液体填充球囊IVRT中，（¹⁶⁶）Ho-EC可能是（¹⁸⁸）Re化合物的可行替代物。