CNS tumors remain among the deadliest forms of cancer, resisting conventional and new treatment approaches, with mortality rates staying practically unchanged over the past 30 years. One of the primary hurdles for treating these cancers is delivering drugs to the brain tumor site in therapeutic concentration, evading the blood–brain (tumor) barrier (BBB/BBTB). Supramolecular nanomedicines (NMs) are increasingly demonstrating noteworthy prospects for addressing these challenges utilizing their unique characteristics, such as improving the bioavailability of the payloads via controlled pharmacokinetics and pharmacodynamics, BBB/BBTB crossing functions, superior distribution in the brain tumor site, and tumor-specific drug activation profiles. Here, we review NM-based brain tumor targeting approaches to demonstrate their applicability and translation potential from different perspectives. To this end, we provide a general overview of brain tumor and their treatments, the incidence of the BBB and BBTB, and their role on NM targeting, as well as the potential of NMs for promoting superior therapeutic effects. Additionally, we discuss critical issues of NMs and their clinical trials, aiming to bolster the potential clinical applications of NMs in treating these life-threatening diseases.

中枢神经系统肿瘤仍然是最致命的癌症之一，对传统和新的治疗方法有抵抗力，在过去 30 年中死亡率几乎没有变化。治疗这些癌症的主要障碍之一是以治疗浓度将药物输送到脑肿瘤部位，从而避开血脑（肿瘤）屏障（BBB/BBTB）。超分子纳米药物 (NM) 越来越多地展示出利用其独特特性应对这些挑战的显着前景，例如通过提高有效载荷的生物利用度  受控的药代动力学和药效学、BBB/BBTB 交叉功能、脑肿瘤部位的优越分布和肿瘤特异性药物激活谱。在这里，我们回顾了基于 NM 的脑肿瘤靶向方法，以从不同的角度展示它们的适用性和翻译潜力。为此，我们概述了脑肿瘤及其治疗、BBB 和 BBTB 的发生率、它们在 NM 靶向中的作用，以及 NM 促进卓越治疗效果的潜力。此外，我们讨论了 NM 及其临床试验的关键问题，旨在加强 NM 在治疗这些危及生命的疾病中的潜在临床应用。