β-细辛醚脂质立方液晶纳米粒的Bottom-up法制备工艺优化及处方筛选  

Bottom-up preparation process optimization and prescription screening for β-asarone lipid cubic liquid crystal nanoparticles

作　　者：李绍林[1] 段启[1] 赵珍东[1] 沈小钟[1] 夏黎[1] 潘颖珊 LI Shao-lin;DUAN Qi;ZHAO Zhen-dong;SHEN Xiao-zhong;XIA Li;PAN Ying-shan(Guang Dong Food and Drug Vocational College,Guangzhou 510520,China)

机构地区：[1]广东食品药品职业学院,广东广州510520

出　　处：《中草药》2021年第24期7464-7472,共9页Chinese Traditional and Herbal Drugs

基　　金：广东省教育厅自然科学基金项目(2017GKQNCX037);广州市科技计划项目(202102080588);广东省医学基金项目(B2021236);广东省中医药局项目(20211280)。

摘　　要：目的以β-细辛醚为模型药物,制备β-细辛醚脂质立方液晶纳米粒(β-asarone lipid cubic liquid crystal nanoparticles,β-A@LCNPs)载药系统。方法采用Bottom-up法,以β-A@LCNPs的包封率、载药量、稳定性常数的归一化综合评分为质量考察指标,分别通过单因素考察立方液晶制备工艺,优化工艺参数,并通过星点设计响应面法,优选β-A@LCNPs最佳处方。结果优选的β-A@LCNPs制备工艺参数为60℃条件下,配置β-A@LCNPs悬浊液,而后1000 r/min匀速搅拌1.5 h,最后置于细胞超声仪,200 W超声15次,每次5 s,间隔10 s;优选的β-A@LCNPs处方为单油酸甘油酯300 mg、β-细辛醚20 mg、聚乙烯醇27000 25 mg、水40 mL。结论β-A@LCNPs制备工艺简单易行,重复性好;所得β-A@LCNPs立方结构形态完整,均一稳定。Objective To prepare β-asarone lipid cubic liquid crystal nanoparticles(β-A@LCNPs) drug delivery system with β-asarone as model drug. Methods The quality of β-A@LCNPs was evaluated by the normalized comprehensive score of encapsulation rate, drug loading capacity and stability constant. The preparation process of cubic liquid crystal was investigated by single factor, and the process parameters were optimized. The optimal formulation of β-A@LCNPs was optimized by response surface method of centroid design. Results The optimal preparation process parameters of β-A@LCNPs were as follows:Bottom-up method, 60 ℃, β-A@LCNPs suspension was prepared, then 1000 r/min uniform stirring for 1.5 h, finally placed in the cell ultrasound instrument, 200 watt ultrasonic power, ultrasonic 15 times, 5 s each time, 10 s interval;The optimal prescription for β-A@LCNPs was glycerin monoleate 300 mg, β-asarone 20 mg, polyvinyl alcohol 27000 25 mg and water 40 m L. Conclusion The preparation process of β-A@LCNPs is simple, easy to perform and has good repeatability. The β-A@LCNPs were homogeneous and stable.

关 键 词：Β-细辛醚 脂质立方液晶 响应面法 纳米粒 Bottom-up法 包封率 载药量 稳定性常数 

分 类 号：R283.6[医药卫生—中药学]