薄荷醇修饰槲皮素脂质体的处方优选及体外靶向性考察

Formulation Optimization and in vitro Targeting of Menthol-modified Quercetin Liposome

目的制备薄荷醇修饰槲皮素脂质体(Men-Qu-Lip)并优化处方,评价其体外靶向性。方法采用薄膜分散法制备Men-Qu-Lip。使用Box-Behnken响应面法,选出Men-Qu-Lip最优处方工艺。采用黄酰罗丹明B(SRB)染色法考察不同给药组对bEnd.3的毒性,用荧光显微镜和流式细胞仪考察其体外靶向性。结果脂质体最优处方为磷脂110 mg、胆固醇30 mg、槲皮素5 mg、水化温度为40℃、处方量为5 mL。槲皮素平均包封率为(91.20±0.53)%。不同组别脂质体在0.012~0.330 mmol/L范围对bEnd.3细胞的细胞活力无显著影响。体外摄取结果表明,经Men修饰的脂质体可以靶向血脑屏障,增加药物入脑量。结论制备并优化了Men-Qu-Lip的处方,经Men修饰的脂质体有较好的靶向性。

Objective To prepare menthol-modified quercetin liposomes,optimize the prescription and evaluate its targeting ability in vitro.Methods Menthol-modified quercetin liposomes were prepared by film dispersion method.Box-Behnken response surface method was used to optimize the optimal prescription technology of menthol-modified quercetin liposome.Sulforhodamine B(SRB)staining method was used to investigate the toxicity of different administration groups to bEnd.3,fluorescence microscopy and flow cytometry were used to investigate it in vitro targeting.Results The optimal formulation of liposome was determined as lecithin 110 mg,cholesterol 30 mg,quercetin 5 mg,hydration temperature was 40℃,and the dosage was 5 mL.The average entrapment efficiency of quercetin was(91.20±0.53)%.The different groups of liposomes in the range of 0.012-0.330 mmol/L had no significant effect on the cell viability of bEnd.3.Cell uptake test in vitro showed that liposomes was modified by menthol target the blood-brain barrier and increased drug delivery to the drain.Conclusion The menthol-modified quercetin liposome is successfully prepared and optimized.The liposome modified by menthol has great targeting.