Preparation of mixed micelles of juglone F127/TPGS and their therapeutic effects on ulcerative colitis
Objective To optimize the preparation process of mixed micelles of juglone F127/D-alpha tocopheryl polythylene glycol succinate(F127/TPGS),and to study the characterization and pharmacodynamics of the mixed micelles.Methods The mixed micelles of juglone F127/TPGS were prepared by thin film dispersion method.With the encapsulation rate as index,single-factor and three-factor and three-level response surface tests were used to optimize the preparation process of walnut quinone mixed micelles.The mixed micelles were characterized by transmission electron microscopy(TEM)and Malvern particle size analyzer.The release of the micelles in vitro was studied by dialysis bag.The anti-ulcerative colitis effect of juglone F127/TPGS mixed micelles in vivo was studied by disease activity index(DAI)and colon HE sections.Results The optimal preparation conditions were as follows:juglone/carrier=1∶50,F127∶ FPGS=4∶5,the hydration volume 10 mL,the hydration time 1 hour,and the ethanol volume 1 mL.After verification,the average encapsulation rate of juglone was 90.53%,which had little deviation from the predicted value of 85.32%.The mixed micelles of juglone F127/TPGS were spherical in shape and uniform in distribution under TEM.The average potential was(-3.86±3.05)mV,the average particle size was(13.91±0.15)nm,and the PDI was(0.092±0.009).The results of release test showed that the cumulative release of F127/TPGS micelles was greater than that of juglone suspension.With the intervention of juglone F127/TPGS mixed micelles,DAI value of mice decreased,the pathological injury of colon tissue was relieved.Conclusion The optimized preparation of juglone F127/TPGS mixed micelles was stable and can increase the solubility of juglone and enhance the anti-ulcerative colitis effect of juglone.
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万方数据
维普
