Preparation, pharmaceutical characterization and in Vitro anti-tumor effects of Aziditaxel-loaded mPEG-PLA micelles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare aziditaxel-loaded mPEG-PLA polymeric micelles, investigate its pharmaceutical characteristics and study its anti-tumor effects in vitro. METHODS: Aziditaxel-loaded polymeric micelles were prepared by thin-film dispersion method. The morphology of aziditaxel-loaded micelles was observed under transmission electron microscope. The particle size distribution and Zeta potential of aziditaxel-loaded micelles were determined by dynamic light scattering method using a Malvern Zetasizer Nano ZS90 analyzer.The technical reproducibility and reconstitution stability of aziditaxel-loaded micelles were also checked. The drug loading and encapsulation efficiency were measured by HPLC. Dialysis method was used to investigate the in vitro release of aziditaxel-loaded micelles, and the release manner was fitted using the mathematic models.The in vitro anti-tumor activities were evaluated by proliferation inhibition and cycle block experiment. RESULTS: Aziditaxel-loaded polymeric micelles were prepared successfully.Aziditaxel-loaded polymeric micelles showed spherical shape with a mean particle size of 24.50 nm, polydispersity index of 0.117 and Zeta potential of -10.06 mV. The mean drug loading and entrapment efficiency were (16.00±0.15)% and (95.80±0.10)%, respectively.The preparation reproducibility was fine, and the reconstitution solution of lyophilized preparation of aziditaxel-loaded polymeric' micelles maintained stable within 6 h.The release behavior of aziditaxel-loaded micelles conformed to the ambiexponent model. Drug-loaded micelles could obviously inhibit the proliferation of MCF-7 breast cancer cell lines in vitro, and induce significant G2/M cycle arrest and apoptosis on MCF-7 cancer cells. CONCLUSION: Aziditaxel-loaded mPEG-PLA polymeric micelles are successfullv prepared. The preparation method is simple, and the pharmaceutical properties of the products conform to the requirements of the subsequent study. The prepared aziditaxel-loaded polymeric micelles exhibit good application prospect with favourable in vitro anti-tumor activities.