Formation and evaluation of docetaxel and triptolide polymer micelles for anti-cancer activity.

AIM

To develop docetaxel (DTX) and triptolide (TPL) polymer micelles (DTX/TPL-PMs) with synergistic anti-cancer effect and to evaluate their anti-cancer activity.

METHODS

DTX/TPL-PMs were prepared by thin-film hydration. The drug loading (DL%), encapsulation efficiency (EE%), and cumulative release rate (CR%) were determined using HPLC. The anti-cancer activity was assessed using CCK-8, inverted microscopy, and laser scanning confocal microscope (LSCM).

RESULTS

DTX/TPL-PMs exhibited the average particle size of 178.58 ± 1.66 nm with a polydispersity index (PDI) of 0.102 ± 0.018 and a zeta potential of 1.19 ± 0.12 mV. These micelles showed a high EE% (89.43%) and a DL% (5.21%). In vitro release studies of DTX/TPL-PMs revealed that the loaded drug exhibited a slow-release phase in physiological fluids and a rapid-release phase under acidic conditions. Compared with the free DTX/TPL drugs, DTX/TPL-PMs were more readily taken up by cancer cells. The cytotoxicity of DTX/TPL-PMs was significantly higher than that of the free drugs, which showed stronger growth inhibitory effects and higher apoptosis rates in cancer cells.

CONCLUSION

The research results demonstrate that DTX/TPL-PMs enhance the therapeutic efficacy against malignancies, while reducing adverse effects. It holds potential as an effective nanotherapeutic for combination chemotherapy and represents a promising clinical strategy.