Institute of Radiopharmaceutical Cancer Research Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden Germany.
Faculty of Chemistry and Food Chemistry Technische Universität Dresden 01062 Dresden Germany.
ChemistryOpen. 2020 Jun 8;9(8):797-805. doi: 10.1002/open.202000126. eCollection 2020 Aug.
The treatment of cancer patients with α-particle-emitting therapeutics continues to gain in importance and relevance. The range of radiopharmaceutically relevant α-emitters is limited to a few radionuclides, as stable chelators or carrier systems for safe transport of the radioactive cargo are often lacking. Encapsulation of α-emitters into solid inorganic systems can help to diversify the portfolio of candidate radionuclides, provided, that these nanomaterials effectively retain both the parent and the recoil daughters. We therefore focus on designing stable and defined nanocarrier-based systems for various clinically relevant radionuclides, including the promising α-emitting radionuclide Ra. Hence, sub-10 nm barium sulfate nanocontainers were prepared and different radiometals like Zr, In, Ba, Lu or Ra were incorporated. Our system shows stabilities of >90 % regarding the radiometal release from the BaSO matrix. Furthermore, we confirm the presence of surface-exposed amine functionalities as well as the formation of a biomolecular corona.
用发射 α 粒子的放射性药物治疗癌症患者的重要性和相关性不断增加。放射药物相关的 α 发射体的范围仅限于少数几个放射性核素,因为缺乏稳定的螯合剂或载体系统来安全地运输放射性货物。将 α 发射体封装到固体无机系统中有助于使候选放射性核素的组合多样化,只要这些纳米材料能有效地保留母体和反冲子体。因此,我们专注于设计各种临床相关放射性核素的稳定且定义明确的基于纳米载体的系统,包括有前途的 α 发射放射性核素 Ra。因此,制备了亚 10nm 的硫酸钡纳米容器,并掺入了不同的放射性金属,如 Zr、In、Ba、Lu 或 Ra。我们的系统显示出从 BaSO 基质中释放放射性金属的稳定性 >90%。此外,我们证实了表面暴露的胺官能团的存在以及生物分子冠的形成。