摘要

The aim was to prepare a compound flexible nanoemulsion co-loaded with cabazitaxel and elemene for the treatment of paclitaxel resistant lung adenocarcinoma. It was prepared successfully. Its average particle size was (102.39 +/- 3.69) nm. The pharmacokinetics in rats revealed that, the AUC((0-t)) and C-max of beta-elemene and cabazitaxel in the compound flexible nanoemulsion had a significant increase of about 5 times than those in the control groups. The pharmacodynamic demonstrated that the compound flexible nanoemulsion (0.625 mg/kg cabazitaxel and 3.125 mg/kg elemene) was better than the cabazitaxel flexible nanoemulsion and cabazitaxel injection (2.5 mg/kg). The LD50 value of cabazitaxel injection was 15.94 mg/kg. The maximum tolerable dose of the compound flexible nanoemulsion was 40 mg/kg. Those results indicated that the compound flexible nanoemulsion co-loaded with cabazitaxel and elemene has a better efficacy and safety on paclitaxel-resistant lung adenocarcinoma, a synergistic effect of reducing toxicity while increasing efficacy.

  • 单位
    杭州师范大学; 广东药学院