Dementia Research Centre, Macquarie Medical School, Faculty of Medicine, Health and Human Sciences, Macquarie University, Sydney, New South Wales, Australia.
J Labelled Comp Radiopharm. 2023 Jul;66(9):237-248. doi: 10.1002/jlcr.4023. Epub 2023 Apr 20.
Trans-blood-brain barrier (BBB) delivery of therapeutic and diagnostic agents is a major challenge in the development of central nervous system (CNS) targeted radiopharmaceuticals. This review is an introduction to the use of peptides as delivery agents to transport cargos into the CNS. The most widely used BBB-penetrating peptides are reviewed here, with a particular emphasis on the broad range of cargos delivered into the CNS using these. Cell-penetrating peptides (CPPs) have been deployed as trans-BBB delivery agents for some time; new developments in the CPP field offer exciting opportunities for the design of next generation trans-BBB complexes. Many of the peptides highlighted here are ready to be combined with diagnostic and therapeutic radiopharmaceuticals to develop highly effective CNS-targeted agents.
血脑屏障（BBB）转运治疗和诊断试剂是开发中枢神经系统（CNS）靶向放射性药物的主要挑战。本综述介绍了使用肽作为递药载体将有效载荷递送至 CNS。本文重点介绍了最广泛使用的穿透血脑屏障的肽，特别强调了使用这些肽递送至 CNS 的广泛有效载荷。细胞穿透肽（CPP）已被用作穿透血脑屏障的递药载体一段时间；CPP 领域的新进展为设计下一代穿透血脑屏障的复合物提供了令人兴奋的机会。本文强调的许多肽都已准备好与诊断和治疗放射性药物结合，以开发高效的中枢神经系统靶向药物。
