目的 研究黄芩苷脂质体的制备工艺。方法 采用逆相蒸发法制备维生素E和聚山梨酯80联合修饰的黄芩苷脂质体,超滤离心分离游离药物,UV测定包封率。在单因素的基础上,采用L16(45)正交实验设计法考察各因素对脂质体包封率的影响,确定黄芩苷脂质体的最佳制备工艺,对该工艺下黄芩苷脂质体进行脂质体粒径和Zeta电位、形貌表征,测定其渗漏率。结果 确定黄芩苷脂质体的最佳工艺条件是:V有机相/ V水相为3∶1,黄芩苷质量浓度3 mg·mL-1,胆固醇与磷脂比为1∶6,维生素E用量2 mg,聚山梨酯80用量120 μL。黄芩苷脂质体平均粒径为52.2 nm,Zeta电位-51.9 mV,包封率70.22％,载药量3.18%。透射电镜结果显示,脂质体的形态良好,大小较为均匀,与激光粒度仪的测定结果一致。放置冰箱保存的黄芩苷脂质体渗漏率低,而室温环境下保存的脂质体渗漏率比较高。细胞抑制研究表明,黄芩苷溶液和黄芩苷脂质体对人急性白血病细胞(HL-60)细胞均有一定的抑制作用,并且随着时间的增加,黄芩苷溶液的抑制作用无明显变化,黄芩苷脂质体的抑制作用大大增加。结论 在逆相蒸发法制备黄芩苷脂质体中,加入维生素E和聚山梨酯80,可提高黄芩苷脂质体的稳定性。
Abstract
OBJECTIVE To study the preparation technology of baicalin glycosides liposomes. METHODS Baicalin liposomes modified by vitamin E and Tween 80 were prepared by reverse phase evaporation method. The free drug was separated by ultracentrifugation and the encapsulation rate was determined by UV spectrophotometry. Based on the results from single factor tests, orthogonal experimental design was used to investigate the factors influencing the envelopment rate of liposomes. The baicalin liposomes prepared by the optimized process were characterized for particle size, Zeta potential, and morphology. RESULTS The optimum conditions for the preparation of liposomes were as follows: the ratio of water phase to organic phase 1∶3, the concentration of baicalin 3 mg·mL-1, the ratio of cholesterol to soy lecithin 1∶6, dosage of vitamin E 2 mg,dosage of Tween 80 120 μL. The mean diameter was 52.2 nm, Zeta potential was -51.9 mV, the encapsulation rate was 70.22% and drug loading capacity was 3.18%. Transmission Electr Microscope(TEM) results showed that the shape of the liposomes was good, the particle size was relatively uniform and consistent with the results of laser granulometry. CONCLUSION The stability of baicalin liposomes can be improved by the addition of vitamin E and Tween 80.
关键词
黄芩苷 /
脂质体 /
逆向蒸发法
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Key words
baicalin /
liposome /
reverse phase evaporation
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中图分类号：
R944
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参考文献
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脚注
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基金
国家自然科学基金项目资助(31302190);泉州市科技科研项目资助(2018Z021);大学生创新训练项目资助(201810399048)
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