Formulation Optimization and in vitro Targeting of Hyaluronic Acid-modified Azithromycin/Quercetin Micelles
Objective To optimize the formulation of hyaluronic acid-modified azithromycin/quercetin micelles and evaluate the active targeting of RAW264.7 cells.Methods The HA modified azithromycin/quercetin micelles were prepared by thin film dispersion method.The Box-Benhken response surface method was used to optimize the three factors affecting the encapsulation efficiency of the micelles(mass ratio of soluplus to quercetin,mass ratio of soluplus to TPGS1000,and hydration temperature),and the encapsulation efficiency of the micelles was verified.The active targeting of the micelles to RAW264.7 cells was examined by fluorescence microscopy and flow cytometry.Results The optimal prescription was determined as Soluplus:Qe=30:1,Soluplus:TPGS=4:1,and the hydration temperature was 40℃.The average encapsulation efficiency of azithromycin and quercetin in hyaluronic acid-modified azithromycin/quercetin micelles was(90.55±1.25)％.The micelle of different groups had no effect on the viability of RAW264.7 cells when the concentration of azithromycin ranged from 0.312 5 to 20 μM.In vitro targeting experiments showed that the HA modified micelles had enhanced targeting ability to RAW264.7 cells.Conclusion The optimal formulation of the micelles has a high encapsulation efficiency,and the HA modified micelles have a good targeting ability to RAW264.7 cells.
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