Silindir-Gunay Mine, Karpuz Merve, Ozer A Yekta
Department of Radiopharmacy, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Department of Radiopharmacy, Faculty of Pharmacy, Izmir Katip Celebi University, Izmir, Turkey.
Cancer Biother Radiopharm. 2020 Aug;35(6):446-458. doi: 10.1089/cbr.2019.3213. Epub 2020 Feb 28.
The rates of cancer incidence and mortality are increasing day by day. Although several conventional methods including surgery, chemotherapy, and radiotherapy (RT) exist for cancer treatment, they are insufficient in the eradication of all tumor tissues and have some side-effects such as narrow therapeutic index and serious side-effects to healthy tissues. Moreover, it may probably recur in time due to the survival and spreading of cancerous cells or any possible metastases. Targeted radionuclide therapy is a promising alternative. α particles are ideal for localized cell killing because of their high linear energy transfer and short ranges. However, upon emission of α particles, the daughter nuclides induce a recoil energy to lead decoupling from any chemical bond that may accumulate in normal tissues. Targeted α therapy can also be performed by targeted delivery systems apart from mAb, mAb fragments, peptides, and small molecules for selective tumor therapy. Targeted drug delivery systems have been developed to overcome the limitations of α therapy. Moreover, drug delivery systems are one of the most searched applications in cancer imaging and/or treatment due to their targeting ability to tumor or biocompatibility properties. The aim of this article is to summarize tumor therapy applications, targeted α RT approach, and to review the role of drug delivery systems in the delivery of α particles for cancer therapy and some instances of targeted α-emitting drug delivery systems from the literature.
癌症的发病率和死亡率日益上升。尽管目前存在包括手术、化疗和放疗(RT)在内的多种传统癌症治疗方法,但这些方法在根除所有肿瘤组织方面并不充分,并且存在一些副作用,如治疗指数窄以及对健康组织有严重副作用。此外,由于癌细胞的存活和扩散或任何可能的转移,癌症可能会及时复发。靶向放射性核素治疗是一种很有前景的替代方法。α粒子因其高线性能量传递和短射程而非常适合局部细胞杀伤。然而,在发射α粒子时,子核素会产生反冲能量,导致与可能在正常组织中积累的任何化学键解耦。除了单克隆抗体(mAb)、mAb片段、肽和小分子用于选择性肿瘤治疗外,靶向α治疗也可通过靶向递送系统来进行。已经开发出靶向药物递送系统以克服α治疗的局限性。此外,由于其对肿瘤的靶向能力或生物相容性,药物递送系统是癌症成像和/或治疗中研究最多的应用之一。本文的目的是总结肿瘤治疗应用、靶向α放疗方法,并从文献中综述药物递送系统在递送α粒子用于癌症治疗中的作用以及一些靶向发射α粒子的药物递送系统实例。