摘要
目的制备包封率高、稳定性好,具有缓释效果的硫酸黄连素多囊脂质体,并对其体外释放进行考察。方法采用复乳法制备硫酸黄连素多囊脂质体,以包封率为指标,采用正交实验优选处方,并考察体外释放及缓释效能。结果制得硫酸黄连素多囊脂质体,显微镜下可见其圆整均匀,内部具有规整囊泡结构;正交设计优选药脂质量比为1∶8,卵磷脂与胆固醇质量比为2∶1,中性磷脂三油酸甘油酯的浓度为70 mmol/L,海藻酸钠的浓度为0.5%,按优选处方制得硫酸黄连素多囊脂质体包封率为85.88%,具有良好缓释效能,72h累积释放度为83.28%,释放曲线符合Weibull模型方程。结论采用复乳法制得硫酸黄连素多囊脂质体圆整均匀,包封率高,具有良好的缓释效能。
Objective To prepare novel berberine sulphate multivesicular liposomes（ BS-MVLs） with high encapsulation efficiency,desirable stability,and sustained release properties. Methods The berberine sulphate multivesicular liposomes were prepared via multiple emulsion method. Orthogonal test was applied for the optimization of the formulation with encapsulation efficiency as the index. Moreover,the in vitro release profiles of BS-MVLs were investigated in physiological saline. Results BS-MVLs were prepared successfully,which were uniform and spherical. Small multivesicular could be clearly observed inside the BS-MVLs. According to the orthogonal test results,the optimal drug/lipid ratio was 1： 8,phosphatidylcholine/cholesterol ratio was 2： 1,concentration of glycerol trioleate was 70 mmol/L and concentration of sodium alginate was 0. 5 %. BS-MVLs with the optimized formulation had encapsulation efficiency as much as 85. 88 % and showed desirable sustained release property. The accumulated release percentage of BS-MVLs was 83. 28 % at 72 h and the correlation equations of release profiles fitted the Weibull model. Conclusion By multiple emulsion method,uniform spherical BS-MVLs with sustained release characteristics could be successfully prepared.
出处
《时珍国医国药》
CAS
CSCD
北大核心
2017年第7期1631-1633,共3页
Lishizhen Medicine and Materia Medica Research
基金
国家自然科学基金(No.81302729)
西南民族大学国家级大学生创新创业训练计划项目(No.201610656072)
关键词
硫酸黄连素
多囊脂质体
缓释
体外释放
正交设计
Berberine sulphate
Multivesicular liposomes
Sustained release
In vitro release
Orthogonal test
