癌症在世界范围内仍然是一种高度致命的疾病。目前，常规的癌症治疗方法或现代免疫疗法均不能准确区分恶性细胞和健康细胞，这导致多种不良副作用的出现。纳米技术的最新进展以及对癌症生物学和纳米生物相互作用的不断增长的认识，推动了一系列纳米载体的开发，旨在通过肿瘤组织、细胞或亚细胞器特异性靶向，提高治疗效果，减少包埋的抗癌药物的非靶向毒性。然而，绝大多数纳米载体并不具备分层靶向能力，它们的治疗指数常常受到肿瘤积累不足、细胞内吞效率低下或亚细胞定位不准确的影响。本综述概述了目前和前景中在设计肿瘤组织、细胞和亚细胞器靶向癌症纳米药物方面的策略，并重点介绍了能够动态整合这三个不同阶段的静态肿瘤靶向的分层靶向技术的最新进展，以最大程度地提高治疗效果。最后，简要讨论了癌症纳米药物的临床应用中当前面临的挑战和未来机遇。©2023.四川大学华西医院。

Cancer remains a highly lethal disease in the world. Currently, either conventional cancer therapies or modern immunotherapies are non-tumor-targeted therapeutic approaches that cannot accurately distinguish malignant cells from healthy ones, giving rise to multiple undesired side effects. Recent advances in nanotechnology, accompanied by our growing understanding of cancer biology and nano-bio interactions, have led to the development of a series of nanocarriers, which aim to improve the therapeutic efficacy while reducing off-target toxicity of the encapsulated anticancer agents through tumor tissue-, cell-, or organelle-specific targeting. However, the vast majority of nanocarriers do not possess hierarchical targeting capability, and their therapeutic indices are often compromised by either poor tumor accumulation, inefficient cellular internalization, or inaccurate subcellular localization. This Review outlines current and prospective strategies in the design of tumor tissue-, cell-, and organelle-targeted cancer nanomedicines, and highlights the latest progress in hierarchical targeting technologies that can dynamically integrate these three different stages of static tumor targeting to maximize therapeutic outcomes. Finally, we briefly discuss the current challenges and future opportunities for the clinical translation of cancer nanomedicines.© 2023. West China Hospital, Sichuan University.