Department of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, Czech Technical University in Prague, Břehová 87/7, 115 19 Prague, Czech Republic.
Department of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, Czech Technical University in Prague, Břehová 87/7, 115 19 Prague, Czech Republic.
Nucl Med Biol. 2024 May-Jun;132-133:108909. doi: 10.1016/j.nucmedbio.2024.108909. Epub 2024 Mar 28.
Radioligand therapy using alpha emitters has gained more and more prominence in the last decade. Despite continued efforts to identify new appropriate radionuclides, the combination of Ac/Bi remains among the most promising. Bismuth-213 has been employed in clinical trials in combination with appropriate vectors to treat patients with various forms of cancer, such as leukaemia, bladder cancer, neuroendocrine tumours, melanomas, gliomas, or lymphomas. However, the half-life of Bi (T = 46 min) implies that its availability for clinical use is limited to hospitals possessing a Ac/Bi radionuclide generator, which is still predominantly scarce. We investigated a new Ac/Bi generator system based on using the composite sorbent α-ZrP-PAN (zirconium(IV) phosphate as active component and polyacrylonitrile as matrix). The developed Ac/Bi generator was subjected to long-term testing after its development. The elution profile was determined and the elution yield, the contamination of the eluate with the parent Ac and the contamination of the eluate with the column material were monitored over time.
The high activity (75 MBq of parent Ac) generator with a length of 75 mm and a diameter of 4 mm containing the composite sorbent α-ZrP-PAN with a particle size of 0.8 to 1.0 mm as the stationary phase, eluted with a mixture of 10 mM DTPA in 5 mM nitric acid, provided Bi with yields ranging from 77 % to 96 % in 2.8 mL of eluate, with parent Ac contamination in the order of 10 %, up to twenty days of use.
All the results of the monitored parameters indicate that the composite sorbent α-ZrP-PAN based separation system for the elution of Bi is a very promising and functional solution.
在过去十年中，使用α发射体的放射性配体疗法越来越受到重视。尽管人们一直在努力寻找新的合适的放射性核素，但 Ac/Bi 的组合仍然是最有前途的组合之一。铋-213 已与适当的载体结合在临床试验中用于治疗各种形式的癌症患者，如白血病、膀胱癌、神经内分泌肿瘤、黑色素瘤、神经胶质瘤或淋巴瘤。然而，铋的半衰期（T=46 分钟）意味着其可用于临床的可用性仅限于拥有 Ac/Bi 放射性核素发生器的医院，而这种发生器仍然主要稀缺。我们研究了一种基于使用复合吸附剂α-ZrP-PAN（磷酸锆作为活性成分和聚丙烯腈作为基质）的新型 Ac/Bi 发生器系统。开发的 Ac/Bi 发生器在开发后进行了长期测试。确定了洗脱曲线，并随时间监测洗脱产率、洗脱液中母体 Ac 的污染以及洗脱液中柱材料的污染。
含有粒径为 0.8 至 1.0 毫米的复合吸附剂α-ZrP-PAN 的 75 毫米长、4 毫米直径的高活性（75MBq 母体 Ac）发生器，以 10mM DTPA 在 5mM 硝酸中的混合物洗脱，提供了 2.8 毫升洗脱液中产率在 77%至 96%之间的 Bi，母体 Ac 的污染率在 10%左右，使用时间长达二十天。
所有监测参数的结果表明，基于复合吸附剂α-ZrP-PAN 的分离系统用于洗脱 Bi 是一种非常有前途和实用的解决方案。
