A Critical Review of Alpha Radionuclide Therapy-How to Deal with Recoiling Daughters?
A Critical Review of Alpha Radionuclide Therapy-How to Deal with Recoiling Daughters?
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DOI：
10.3390/ph8020321
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发表时间：
2015-06-10
期刊：
影响因子：
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通讯作者：
Denkova AG
中科院分区：
文献类型：
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作者：
de Kruijff RM;Wolterbeek HT;Denkova AG
本文综述了α放射性核素治疗的成功和目前面临的挑战。与β或γ辐射相比，α粒子在杀死肿瘤细胞方面具有优势，这是由于它们的穿透深度短和线性能量传递（LET）高。本文简要介绍了仅发射一个α粒子的放射性核素的临床成功，主要关注在衰变链中具有多个α发射子体的α发射放射性核素。虽然具有较长半衰期的优点，但放射性核素如224Ra（镭），223Ra和225Ac（锕）的反冲子体在不保留在肿瘤部位时会对健康组织造成重大损害。三种不同的方法来处理这个问题进行了讨论：封装在纳米载体中，快速摄取的α发射放射性核素在肿瘤细胞中，和本地管理。每种方法都有其优点和缺点，但当需要在临床上使用更大的活性时，纳米载体似乎是减少毒性作用的最有前途的解决方案，前提是在健康组织中没有积累。
This review presents an overview of the successes and challenges currently faced in alpha radionuclide therapy. Alpha particles have an advantage in killing tumour cells as compared to beta or gamma radiation due to their short penetration depth and high linear energy transfer (LET). Touching briefly on the clinical successes of radionuclides emitting only one alpha particle, the main focus of this article lies on those alpha-emitting radionuclides with multiple alpha-emitting daughters in their decay chain. While having the advantage of longer half-lives, the recoiled daughters of radionuclides like 224Ra (radium), 223Ra, and 225Ac (actinium) can do significant damage to healthy tissue when not retained at the tumour site. Three different approaches to deal with this problem are discussed: encapsulation in a nano-carrier, fast uptake of the alpha emitting radionuclides in tumour cells, and local administration. Each approach has been shown to have its advantages and disadvantages, but when larger activities need to be used clinically, nano-carriers appear to be the most promising solution for reducing toxic effects, provided there is no accumulation in healthy tissue.