脑胶质瘤是最常见的神经系统恶性肿瘤。针对脑胶质瘤的主动靶向治疗是世界性难题。以胶质瘤多个环节为靶点的多功能靶向纳米递药系统研究正受到广泛关注。本课题利用Pep-1肽对胶质瘤细胞和CGKRK肽对胶质瘤新生血管的特异性归巢能力，将聚乙二醇-聚乳酸-羟基乙酸嵌段共聚物(PLGA-PEG)纳米粒同时用Pep-1肽和CGKRK肽进行共修饰，构建针对胶质瘤细胞和胶质瘤新生血管的多靶点靶向纳米递药系统，特异性地将药物同时递送到胶质瘤细胞和胶质瘤新生血管内皮细胞。一方面通过破坏胶质瘤血管，切断胶质瘤的营养供应链，"饿死"胶质瘤细胞和组织。另一方面，将药物直接导入胶质瘤细胞与之接触，直接杀死胶质瘤细胞和组织。从而提高胶质瘤的治疗效果，降低给药剂量，减轻毒副作用。本研究可为从制剂角度通过载体系统来寻求多靶点抗胶质瘤提供新思路和新方法，对最终攻克脑胶质瘤具有积极意义。

Glioma is the most common malignant tumor of the nervous system. Active targeted therapy against glioma is a worldwide problem. It is widespreadly concerned of the research on multi-target therapy of glioma basing on multifunctional target nano drug delivery system. Because of the specific homing ability between Pep-1 peptide and glioma cells as well as between CGKRK peptide and glioma neovascular, polyethylene glycol-polylactic acid-glycolic acid block copolymers (PLGA-PEG) nanoparticles were decorated with both Pep-1 peptide and CGKRK peptide to develop multiple targeted nano-drug delivery system in this study. Therefore, drugs loaded into the multiple targeted nano-drug delivery system could be delivered into glioma cells and glioma neovascular endothelial cells simultaneously. The anti-glioma effects are cooperated by two aspects. One is the destruction of glioma blood vessels, cutting the glioma nutrition supply chain and "starving to death" of glioma cells and tissues. The other aspect is that the drugs are directly imported into glioma cells by the multiple targeted nano-drug delivery system and kill glioma cells or glioma tissues. Thereby it can improve the therapeutic effect and reduce dosage, reduce side effects of chemotherapy drugs. This study can provide one novel target strategy of glioma treatment through drug carrier system of pharmaceutics, which is of positive significance to eventually overcome glioma.