WANG Chengde,XU Yunqiu,SU Zhipeng. Preparation, characterization of micheliolide DSPE-PEG nanomicelles and its induction of apoptosis in glioma cells[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2022, 52(8): 613-619.
Abstract：Objective: To prepare and characterize micheliolide-loaded polyethylene glycol-derivatized phosphatidyle-thanolamine (MCL@DSPE-PEG) nanomicelles, and evaluate its anti-tumor effect on tumor cells. Methods: MCL@DSPE-PEG nanomicelles were prepared by film hydration method, and their appearance characteristics were observed. The particle size, polydispersion coefficient (PDI), drug-loading amount and encapsulation efficiency of the nanomicelles were detected. The drug release of MCL@DSPE-PEG nanomicelles in pH 7.4 phosphate buffer were compared within 0-144 h. The U87 and U251 glioma cells were divided into model group and MCL@DSPE-PEG nanomicelles group. Cell viability and apoptosis were evaluated. The expressions of apoptosis related protein including Caspase3, Caspase8 and Bcl-2 were detected. Results: The morphology of MCL@DSPE-PEG nanomicelles were uniform ellipsoidal shape. The particle size was (123.8±0.5) nm and PDI was 0.236±0.005. The drug-loading amount was 8.96%±0.56%, encapsulation efficiency was 85.49%±3.66%. Accumulative release rate was 73.30% within 144 h. MCL raw material was released completely within 48 h. MCL@DSPE-PEG nanomicelles inhibited the growth and cell cloning of U87 and U251 glioma cells. Compared with the model group, the expression of Bcl-2 protein was significantly decreased, while the expression of Caspase3 and Caspase8 protein were dramatically increased (P<0.05 respectively). Conclusion:MCL@DSPE-PEG nanomicelles are prepared successfully, which can induce apoptosis of U87 and U251 glioma cells and inhibit tumor growth.
