Li Jianru, Zhang Zixia, Zhang Baoli, Yan Xiyun, Fan Kelong
CAS Engineering Laboratory for Nanozyme, Key Laboratory of Protein and Peptide Pharmaceutical, Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, P. R. China.
Nanozyme Medical Center, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450052, China.
Biomater Sci. 2023 May 16;11(10):3394-3413. doi: 10.1039/d2bm02152h.
Achieving effective drug delivery to traverse the blood-brain barrier (BBB) and target tumor cells remains the greatest challenge for brain tumor therapy. Importantly, the overexpressed membrane receptors on the brain endothelial cells, especially transferrin receptor 1 (TfR1), which mediate their ligands/antibodies to overcome the BBB by transcytosis, have been emerging as promising targets for brain tumor therapy. By employing ligands (, transferrin, H-ferritin), antibodies or targeting peptides of TfR1 or aptamers, various functional nano-formulations have been developed in the last decade. These agents showed great potential for the treatment of brain diseases due to their ideal size, high loading capacity, controlled drug release and suitable pharmacokinetics. Herein, we summarize the latest advances on TfR1-targeted nanomedicine for brain tumor therapy. Moreover, we also discuss the strategies of improving stability, targeting ability and accumulation of nano-formulations in brain tumors for better outcomes. In this review, we hope to provide inspiration for the rational design of TfR1-targeted nanomedicine against brain tumors.
实现有效的药物递送以穿越血脑屏障（BBB）并靶向肿瘤细胞仍然是脑肿瘤治疗面临的最大挑战。重要的是，脑内皮细胞上过度表达的膜受体，特别是转铁蛋白受体1（TfR1），其通过转胞吞作用介导其配体/抗体克服血脑屏障，已成为脑肿瘤治疗的有希望的靶点。在过去十年中，通过使用TfR1的配体（如转铁蛋白、H-铁蛋白）、抗体或靶向肽或适体，已经开发了各种功能性纳米制剂。这些药物因其理想的尺寸、高负载能力、可控的药物释放和合适的药代动力学而显示出治疗脑部疾病的巨大潜力。在此，我们总结了用于脑肿瘤治疗的TfR1靶向纳米药物的最新进展。此外，我们还讨论了提高纳米制剂在脑肿瘤中的稳定性、靶向能力和积累的策略，以获得更好的治疗效果。在这篇综述中，我们希望为针对脑肿瘤的TfR1靶向纳米药物的合理设计提供灵感。
