Preparation and evaluation in vitro and in vivo of α-hederin-loaded polymer micelles
Objective To prepare α-hederin-loaded polymer micelles(α-Hed-PMs)and evaluate its inhibition effect on HepG2 cells.Methods The α-Hed-PMs were prepared by solvent evaporation-thin film hydration dispersion method using Pluronic F127 and TPGS as carrier materials.The formulation composition of α-Hed-PMs was determined by comprehensive evaluation of particle size distribution,Zeta potential and encapsulation efficiency.The critical micelle concentration of polymer micelles was determined.The microstructure of α-Hed-PMs was observed under transmission electron microscope.The presence status of α-Hed in micelles was determined by DSC.The stability and drug release rate of α-Hed-PMs in medium solution with different pH values(5.0,6.0 and 7.4)were investigated.The inhibition effect of α-Hed and α-Hed-PMs(4,8,16,32,and 64 μg·mL-1)were compared in vitro and in vivo.HepG2 tumor bearing mice were prepared,and the effects of 0.9％sodium chloride solution(control group),α-Hed and α-Hed-PMs(dose of 30 mg·kg-1)on tumor volume were investigated.Results The optimal composition of α-Hed-PMs was as follows:the mass ratio of Pluronic F127 to TPGS was 6∶1.The critical micelle concentration was 0.031 mg·mL-1.The spherical distribution of α-Hed-PMs could be observed under transmission electron microscope.The results of DSC showed that α-Hed existed in amorphous form in micelles.After dilution with pH 5.0,6.0,and 7.4 buffer solutions,α-Hed PMs showed no flocculation or precipitation within 24 hours,and their particle size remained largely unchanged.The α-Hed raw material was basically completely released within four hours,the drug release rate of α-Hed-PMs in different pH values was faster in the early stage and gentle in the late stage,with almost complete release after 50 hours.The results of in vivo and in vitro showed that α-Hed-PMs had better inhibitory effect on HepG2 cells than α-hederin.Conclusion In this study,α-Hed was prepared into polymer micelles using Pluronic F127 and TPGS as carrier materials,which could achieve better anti-tumor effect.
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维普
