Mdanda Sipho, Ngema Lindokuhle M, Mdlophane Amanda, Sathekge Mike M, Zeevaart Jan Rijn
Nuclear Medicine Research Infrastructure (NuMeRI), Steve Biko Academic Hospital, Pretoria 0028, South Africa.
Department of Nuclear Medicine, University of Pretoria, Pretoria 0001, South Africa.
Pharmaceutics. 2023 Jun 13;15(6):1719. doi: 10.3390/pharmaceutics15061719.
The actinium-225 (Ac) radioisotope exhibits highly attractive nuclear properties for application in radionuclide therapy. However, the Ac radionuclide presents multiple daughter nuclides in its decay chain, which can escape the targeted site, circulate in plasma, and cause toxicity in areas such as kidneys and renal tissues. Several ameliorative strategies have been devised to circumvent this issue, including nano-delivery. Alpha-emitting radionuclides and nanotechnology applications in nuclear medicine have culminated in major advancements that offer promising therapeutic possibilities for treating several cancers. Accordingly, the importance of nanomaterials in retaining the Ac daughters from recoiling into unintended organs has been established. This review expounds on the advancements of targeted radionuclide therapy (TRT) as an alternative anticancer treatment. It discusses the recent developments in the preclinical and clinical investigations on Ac as a prospective anticancer agent. Moreover, the rationale for using nanomaterials in improving the therapeutic efficacy of α-particles in targeted alpha therapy (TAT) with an emphasis on Ac is discussed. Quality control measures in the preparation of Ac-conjugates are also highlighted.
锕-225（Ac）放射性同位素在放射性核素治疗中的应用具有极具吸引力的核性质。然而，Ac放射性核素在其衰变链中会产生多个子核素，这些子核素可能会逃离靶位点，在血浆中循环，并在肾脏和肾组织等部位造成毒性。已经设计了几种改善策略来规避这个问题，包括纳米递送。发射α粒子的放射性核素和纳米技术在核医学中的应用取得了重大进展，为治疗多种癌症提供了有前景的治疗可能性。因此，纳米材料在阻止Ac子核反冲进入非靶器官方面的重要性已得到确立。本综述阐述了靶向放射性核素治疗（TRT）作为一种替代抗癌治疗方法的进展。它讨论了Ac作为一种潜在抗癌剂在临床前和临床研究中的最新进展。此外，还讨论了使用纳米材料提高α粒子在靶向α治疗（TAT）中的治疗效果的基本原理，重点是Ac。还强调了Ac缀合物制备中的质量控制措施。
