Glioma is one of the deadliest intrinsic brain tumours due to its invasive growth. The effect of glioma treatment is poor because of the presence of the blood-brain barrier and blood tumour barrier and insufficient drug targeting. DNA tetrahedrons (TDN) show great potential for drug delivery and may be a novel therapeutic strategy for glioma. In this study, we used TDN to deliver doxorubicin (DOX) for the glioma therapy. Gint4.T, an aptamer that could recognize platelet-derived growth factor receptor β on tumour cell, was used to modify TDN (Apt-TDN) for targeted drug delivery. The TDN were self-assembled by one-step synthesis, which showed small size (10 nm) and negative charge. Fetal bovine serum test showed its stability as a drug delivery vehicle. Apt-TDN could be effectively taken up by U87MG cells. Compared with DOX and DOX@TDN (TDN loaded with DOX), the DOX@Apt-TDN (Gint4.T-modified TDN loaded with DOX) showed more early apoptosis rate, higher cell cycle arrest, and greater cytotoxicity towards U87MG cells. In conclusion, our findings indicated that DOX@Apt-TDN provides a novel therapy with promising clinical application for gliomas patients.

脑胶质瘤由于其侵袭性生长而成为最致命的固有脑肿瘤之一。由于存在血脑屏障和血液肿瘤屏障，并且药物靶向不足，因此胶质瘤治疗效果差。DNA四面体（TDN）显示出巨大的药物输送潜力，可能是神经胶质瘤的一种新型治疗策略。在这项研究中，我们使用TDN运送阿霉素（DOX）用于神经胶质瘤治疗。Gint4.T是一种能够识别肿瘤细胞上血小板源性生长因子受体β的适体，被用于修饰TDN（Apt-TDN）以进行靶向药物递送。TDN通过一步合成自组装，显示出小尺寸（10 nm）和负电荷。胎牛血清测试显示出其作为药物递送载体的稳定性。U87MG细胞可以有效地吸收Apt-TDN。与DOX和DOX @ TDN（装载有DOX的TDN）相比，DOX @ Apt-TDN（装载有DOX的Gint4.T修饰的TDN）显示出更高的早期凋亡率，更高的细胞周期停滞以及对U87MG细胞的更大细胞毒性。总之，我们的发现表明，DOX @ Apt-TDN为神经胶质瘤患者提供了一种新的疗法，具有广阔的临床应用前景。