Objective Developed the core-matched nanoemulsions (CMNEs) to co-delivery paclitaxel-oleic acid prodrug (PTX-OA) and brucea javanica oil (BJO) for increasing the antitumor effect.. Methods Antitumor effects and mechanism of PTX-OA/BJO CMNEs that the combination therapy which based on core-matched technology (CMT) were evaluated in vitro and in vivo. Results The PTX-OA/BJO CMNEs were of nanoscale particle size (108.7 ± 2.3) nm and with entrapment efficiency of > 95%. The PTX-OA/BJO CMNEs displayed concentration and time-dependent cytotoxicity against HepG-2 cells and increased G2/M phase block. More importantly, a significant reduction of the tumor volume with no obvious toxicity was observed in nude mice model following administration of PTX-OA/BJO CMNEs compared with the control treated with normal saline (P < 0.05), which suggested the excellent efficacy in vivo. It was further found that the enhanced effectiveness of PTX-OA/BJO CMNEs were associated with the ability of inducing apoptosis of the tumor cells, as well as obviously inhibiting tumor cell proliferation and the activity of TOPO Ⅱ. Conclusion Co-encapsulation of two drugs with different mechanisms allows simultaneous interruption of diverse anticancer pathways, resulting in increased therapeutic response and lower toxicity.
关键词:
紫杉醇;鸦胆子油;分子配型纳米乳;癌症;联合治疗
Keywords:
Project Supported:
National Nature Science Foundation of China (81403109) and Science and Technology Planning Project of Guangdong Province (2014A020210021, 2016A020217017)
Shu-qing Cao, Kuan-yun Zhang, Xia Yan, Yan Ma. Preparation and evaluation of Paclitaxel and Brucea Javanica oil core-matched nanoemulsions to treat cancer in vitro and in vivo[J]. Chinese Herbal Medicines (CHM),2018,10(3):310-317
