Vascular endothelial growth factor (VEGF) has been implicated as the key regulator of tumor neovascularization. RNAi interference plays a critical role on down-regulation of VEGF, while single VEGF inhibition could not completely suppress angiogenesis and tumor growth; the effect of siRNA is temporary. To improve glioma therapy efficacy, an angiopep-2 (Ap) modified redox-responsive glycolipid-like copolymer co-delivering siVEGF and paclitaxel (PTX), termed as Ap-CSssSA/P/R complexes, was developed in this study. Ap modification significantly enhanced the distribution of Ap-CSssSA in glioma cells both in vitro and in vivo. Ap-CSssSA/P/R complexes could simultaneously deliver siVEGF and PTX into tumor cells, exhibiting great superiority in glioma growth suppression via receptor-mediated targeting delivery and cell apoptosis, accompanied with an obvious inhibition of neovascularization induced by VEGF gene silencing. The present study indicated that the combination delivery of siVEGF and PTX via Ap-modified copolymeric micelles presented a promising and safe platform for glioma targeted therapeutics.

血管内皮生长因子（VEGF）被认为是肿瘤新血管形成的关键调节因子。RNAi干扰在VEGF的下调中起关键作用，而单一VEGF的抑制不能完全抑制血管生成和肿瘤的生长。siRNA的作用是暂时的。为了提高神经胶质瘤的治疗功效，在这项研究中开发了一种血管生成蛋白2（Ap）修饰的氧化还原反应性糖脂样共聚物，共同递送siVEGF和紫杉醇（PTX），称为Ap-CSssSA / P / R复合物。鸭修改显著增强AP-CSssSA的神经胶质瘤细胞中的分布两者在体外和体内。Ap-CSssSA / P / R复合物可以同时将siVEGF和PTX递送到肿瘤细胞中，通过受体介导的靶向递送和细胞凋亡在神经胶质瘤生长抑制方面显示出极大的优势，同时明显抑制了VEGF基因沉默诱导的新血管形成。本研究表明，通过Ap修饰的共聚胶束联合递送siVEGF和PTX为胶质瘤靶向治疗提供了一个有希望且安全的平台。