摘要
目的制备柚皮素脂质体,优化其处方和工艺,并对其相关性能进行评价。方法采用乙醇注入法制备柚皮素脂质体,通过正交设计优化处方工艺;利用马尔文动态光散射粒径测定仪测定其zeta电位和粒径,采用微型凝胶柱离心法分离游离药物和脂质体,HPLC法测定脂质体中柚皮素的包封率。结果确定最佳处方为:磷脂的质量浓度为0.006 g·m L^(-1),胆固醇与磷脂的质量比为1∶3,药脂比为1∶20,缓冲液p H值为7.40,类脂溶液的溶解温度设定为55℃,类脂溶液的溶解时间为25 min。制得的柚皮素脂质体包封率为(80.44±0.98)%,平均粒径为(223±11)nm,Zeta电位为(-35.9±5)m V。结论乙醇注入法制备柚皮素脂质体工艺简单可行,所制备的柚皮素脂质体包封率高、粒径较小、稳定性好。
Objective To prepare naringenin liposome（NRG-LIP）, optimize the prescription and technological conditions, and evaluate relative performance. Methods NRG-LIP was prepared by ethanol injection method, and orthogonal design was adopted to screen the optimal conditions. The particle sizes and zeta potential were detected by Zetasizer Nano, while the encapsulation efficiency of NRG-LIP was determined by HPLC after the free drug was separated by Mini gel centrifugation method. Results The optimal technological conditions of NRG-LIP were as follows： the concentration of phospholipid was 0.006 g·m L-（-1）, the mass ratio of cholesterol to phospholipid was 1 ∶ 3, the ratio of naringenin to lecithin was 1 ∶ 20, pH value of PBS buffer solution was 7.40, the temperature of dissolved lipid solution was 55 ℃, the dissolution time of lipid solution was 25 min. The encapsulation efficiency of the prepared liposome was（80.44±0.98）%, the average particle size was（223±11） nm, and Zeta potential was（- 35.9±5） m V. Conclusion NRG-LIP by ethanol injection method is simple and feasible. The prepared NRG-LIP have a high encapsulation efficiency, smaller particle size and stable.
出处
《中南药学》
CAS
2015年第12期1266-1269,共4页
Central South Pharmacy
基金
国家自然科学基金面上项目(No.81473424)
关键词
脂质体
乙醇注入法
柚皮素
包封率
liposome
ethanol injection method
naringenin
entrapment efficiency
