Graphene and its derivatives with exceptional properties are being exploited for drug delivery and even combined therapies for enhanced antitumor activity and reduced side effects. However, the unfavorable surface chemistry of pristine graphene and reduced graphene oxide made them take covalent and non-covalent functionalization strategies to improve their biocompatibility. Although graphene oxide (GO) is soluble in water owing to its oxygen-containing groups such as carboxylic acid and hydroxyl groups, it is highly accepted when to be modified to improve its colloidal stability in physiological buffers in the presence of salts. In this work, we functionalized GO with Pluronic F127 molecules via non-covalent interaction and found that GO and PF127/GO nanohybrid with a concentration lower than 5 μg/ml have no obvious toxic effect on human astrocytes (AS) and human glioma (U251) cells. Anti-tumor drug doxorubicin (DOX) being loaded onto the PF127/GO nanocarriers by π-π stacking exhibited a high loading capacity of 0.83 mg/mg and loading efficiency of 83%. Our study confirmed that the PF127/GO/DOX (PGD) induced a higher apoptosis rate (12.27 ± 0.06%) of U251 cells than that of free DOX (8.20 ± 0.06%) (P < 0.05). Western blotting results indicated that PGD affected the MAPK signaling pathway and induced the intrinsic pathway of apoptosis for the activation of Caspase-3 in U251 cells, which may provide more evidence for the signal pathway of tumor-targeting therapy.

石墨烯及其具有优异性能的衍生物已被用于药物输送，甚至用于增强抗肿瘤活性和减少副作用的联合疗法。然而，原始石墨烯和还原的氧化石墨烯的不利表面化学性质使它们采取共价和非共价官能化策略来提高其生物相容性。尽管氧化石墨烯（GO）由于其诸如羧酸和羟基的含氧基团而可溶于水，但是当在盐的存在下对其进行修饰以改善其在生理缓冲液中的胶体稳定性时，氧化石墨烯（GO）被广泛接受。在这项工作中 我们通过非共价相互作用用Pluronic F127分子对GO进行功能化，发现GO和PF127 / GO纳米杂交物的浓度低于5μg/ ml对人星形胶质细胞（AS）和人神经胶质瘤（U251）细胞没有明显的毒性作用。通过π-π堆积将抗肿瘤药物阿霉素（DOX）装载到PF127 / GO纳米载体上显示出0.83 mg / mg的高装载量和83％的装载效率。我们的研究证实PF127 / GO / DOX（PGD）诱导的U251细胞凋亡率（12.27±0.06％）高于游离DOX（8.20±0.06％）（P  <0.05）。Western blotting结果表明，PGD影响了UAPK细胞中MAPK信号通路并诱导了凋亡的内在途径激活了Caspase-3的活化，这可能为肿瘤靶向治疗的信号通路提供了更多的证据。