Despite chemotherapy has been widely used for tumor therapy, the serious side effect is still a major challenge. Recently, two dimensional nanomaterial-based drug delivery systems have attracted wide concern due to their high drug loading and low side effect. In addition, some kinds of nanomaterials can directly act as a photosensitizer to induce cancer destruction. In this study, we developed a drug delivery system of mixture of high/low molecular weight branched polyethylenimine-polyethylene glycol-reduced graphene oxide (mBPEI-PEG-rGO) using reduced graphene oxide as matrix. A model drug of doxorubicin (DOX) was loaded on the nanocomposites with the efficiency of 81% and the release rate of more than 50% at acidic environment. In vitro experiments indicated that mBPEI-PEG-rGO-DOX with enhanced stability and biocompatibility efficiently delivered and released DOX into cells mainly through micropinocytosis and killed SMMC-7721 cells by inducing reactive oxygen species (ROS) and cell apoptosis. Furthermore, in vivo experiments indicated that the combination of intratumoral injection of mBPEI-PEG-rGO-DOX and local laser irradiation nearly ablated hepatocarcinoma. In conclusion, this new drug delivery system provided an alternative for combinational photothermal and chemotherapy against hepatocarcinoma.

尽管化学疗法已广泛用于肿瘤治疗，但严重的副作用仍然是一个重大挑战。近年来，基于二维纳米材料的药物递送系统因其高载药量和低副作用而受到广泛关注。此外，某些种类的纳米材料可以直接作为光敏剂诱导癌症破坏。在这项研究中，我们开发了一种以还原氧化石墨烯为基质的高/低分子量支化聚乙烯亚胺-聚乙二醇还原氧化石墨烯 (mBPEI-PEG-rGO) 混合物的给药系统。一种模型药物阿霉素 (DOX) 负载在纳米复合材料上，在酸性环境下的效率为 81%，释放率超过 50%。体外实验表明，具有增强稳定性和生物相容性的 mBPEI-PEG-rGO-DOX 主要通过微胞饮作用有效地将 DOX 递送和释放到细胞中，并通过诱导活性氧 (ROS) 和细胞凋亡来杀死 SMMC-7721 细胞。此外，体内实验表明，瘤内注射 mBPEI-PEG-rGO-DOX 和局部激光照射的组合几乎消融了肝癌。总之，这种新的药物输送系统为光热和化学疗法联合治疗肝癌提供了一种替代方案。体内实验表明，瘤内注射 mBPEI-PEG-rGO-DOX 和局部激光照射的组合几乎消融了肝癌。总之，这种新的药物输送系统为光热和化学疗法联合治疗肝癌提供了一种替代方案。体内实验表明，瘤内注射 mBPEI-PEG-rGO-DOX 和局部激光照射的组合几乎消融了肝癌。总之，这种新的药物输送系统为光热和化学疗法联合治疗肝癌提供了一种替代方案。