Due to the special physiological and pathological characteristics of gliomas, most therapeutic drugs are prevented from entering the brain. To improve the poor prognosis of existing therapies, researchers have been continuously developing non-invasive methods to overcome barriers to gliomas therapy. Although these strategies can be used clinically to overcome the blood‒brain barrier (BBB), the accurate delivery of drugs to the glioma lesions cannot be ensured. Nano-drug delivery systems (NDDS) have been widely used for precise drug delivery. In recent years, researchers have gathered their wisdom to overcome barriers, so many well-designed NDDS have performed prominently in preclinical studies. These meticulous designs mainly include cascade passing through BBB and targeting to glioma lesions, drug release in response to the glioma microenvironment, biomimetic delivery systems based on endogenous cells/extracellular vesicles/protein, and carriers created according to the active ingredients of traditional Chinese medicines. We reviewed these well-designed NDDS in detail. Furthermore, we discussed the current ongoing and completed clinical trials of NDDS for gliomas therapy, and analyzed the challenges and trends faced by clinical translation of these well-designed NDDS.

由于胶质瘤特殊的生理和病理特征，大多数治疗药物都无法进入大脑。为了改善现有疗法的不良预后，研究人员一直在不断开发非侵入性方法来克服胶质瘤治疗的障碍。尽管这些策略可以在临床上用于克服血脑屏障（BBB），但不能确保将药物准确输送到胶质瘤病灶。纳米药物递送系统（NDDS）已被广泛用于精确药物递送。近年来，研究人员集思广益，攻克难关，许多精心设计的NDDS在临床前研究中表现突出。这些精心设计主要包括级联通过BBB和靶向胶质瘤病灶，响应胶质瘤微环境的药物释放，基于内源性细胞/细胞外囊泡/蛋白质的仿生递送系统，以及根据中药活性成分创建的载体。我们详细回顾了这些精心设计的 NDDS。此外，我们讨论了当前正在进行和已完成的 NDDS 用于胶质瘤治疗的临床试验，并分析了这些精心设计的 NDDS 临床转化所面临的挑战和趋势。