The co-delivery of chemotherapeutic drugs and siRNA has gained increasing attentions owing to the enhanced antitumor efficacy over single administration. In this work, a chitosan-based pH-responsive prodrug vector was developed for the co-delivery of doxorubicin (DOX) and Bcl-2 siRNA. The accumulation of fabricated nanoparticles in hepatoma cells was enhanced by glycyrrhetinic acid receptor-mediated endocytosis. The cumulative release amount of the encapsulated DOX and siRNA reached 90.2 % and 81.3 % in 10 h, respectively. More strikingly, this nanoplatform can efficiently integrate gene- and chemo-therapies with a dramatically enhanced tumor inhibitory rate (88.0 %) in vivo. This co-delivery system may provide the latest strategy to meet the needs of combination therapies for tumors, offering safe and efficient improvements to the synergistic antitumor efficacy of gene-chemotherapies.

由于与单次给药相比增强的抗肿瘤功效，化学治疗药物和siRNA的共同给药越来越受到关注。在这项工作中，开发了一种基于壳聚糖的pH响应前药载体，用于共递送阿霉素（DOX）和Bcl-2 siRNA。甘草次酸受体介导的内吞作用增强了肝癌细胞中纳米颗粒的积累。包封的DOX和siRNA在10小时内的累积释放量分别达到90.2％和81.3％。更惊人的是，这种纳米平台可以有效地整合基因和化学疗法，并在体内显着提高肿瘤抑制率（88.0％）。 该共同递送系统可以提供满足肿瘤联合疗法需求的最新策略，为基因化学疗法的协同抗肿瘤功效提供安全有效的改善。