Formulation Optimization of Bingpian(Borneol)Modified Schisandrin B Micelles and Their Effect on Targeting Evaluation in Vitro of bEnd.3 Cell
Objective To optimize the formulation of Bingpian(Borneol)modified Schisandrin B micelles(Borneol-Schisan-drin B-Micelles,Bor-Sch B-Ms)and preliminarily evaluate their brain targeting effect in vitro.Methods Bor-Sch B-Ms were prepared by thin film dispersion method.The three factors of Soluplus/TPGS1000 mass ratio(mg/mg),Soluplus/Schisandrin B mass ratio(mg/mg)and hydration temperature(℃)were investigated.The optimal formulation and preparation process of Bor-Sch B-Ms were determined by Box-Behnken design response surface method,and the micelles prepared by the optimal formulation process were characterized.The content of Schisandrin B in micelles was determined by high performance liquid chro-matography(HPLC)to measure the entrapment efficiency of Bor-Sch B-Ms.The targeting ability of Bor-Sch B-Ms in vitro was appraised by the fluorescence uptake experiment of different medications on the vascular endothelial cells(bEnd.3)in the mouse brain.Results The first-best prescription was Soluplus 120 mg,Soluplus/TPGS1000=2∶1,Soluplus/Schisandrin B=12∶1,DSPE-PEG2000 2 mg,hydration temperature 40℃ and prescription dosage 5 mL.The particle size of the optimal micelles was(93.72±0.65)nm,the potential was(-2.73±0.35)mv,and the entrapment efficiency of Bor-Sch B-Ms was(93.54± 0.86)％.In vitro cell uptake experiment showed that the fluorescence intensity of cells in Bor-Sch B-Ms group was signifi-cantly higher than that in Sch B-Ms group(P＜0.05).Conclusion The first-best prescription of Bor-Sch B-Ms was screened by Box-Behnken design response surface method and the prepared Bor-Sch B-Ms have certain potential brain targe-ting.
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