芦荟大黄素与川芎嗪纳米脂质体的制备及工艺条件优化  

Preparation and optimization of aloe emodin and ligustrazine nanoliposomes

作　　者：唐佳梅 宋佳文 郭力[1] TANG Jiamei;SONG Jiawen;GUO Li(School of Pharmacy,State Key Laboratory of Southwestern Chinese Medicine Resources,Chengdu University of Traditional Chinese Medicine,Sichuan Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院,西南特色中药资源国家重点实验室,四川成都611137

出　　处：《中药与临床》2025年第1期17-22,共6页Pharmacy and Clinics of Chinese Materia Medica

基　　金：四川省科技基础条件平台项目(2019JDPT0032);“杏林学者”学科人才科研提升计划(CXTD2018012)。

摘　　要：目的:制备芦荟大黄素-川芎嗪脂质体纳米粒(Aloe emodin-tetramethylpyrazine liposome nanoparticles,AETMP-Lip),优化该处方并确定AE-TMP-Lip的最佳工艺条件。方法:采用薄膜分散法来制备脂质体,用紫外分光光度法测定AE、TMP的紫外吸光度,以溶剂选择、溶剂用量、温度等单因素为考察因素,脂质体中药物含量为指标,通过星点设计-效应面法优化处方及制备工艺,并对其进行验证。结果:成膜温度为45℃项下的温度变化、超纯水的用量以及成膜溶剂用量对脂质体的含量影响最大,采用三因素三水平的星点设计实验方案确定了最佳的工艺优化条件。结论:确定芦荟大黄素与川芎嗪用量各1 mg、大豆卵磷脂30 mg、胆固醇10 mg、吐温-8013 mg,三氯甲烷-甲醇为4∶1的有机溶剂,溶解,超声,在成膜温度45℃的条件下旋转减压蒸发,待成膜完全后,调节水化温度为35℃,加入超纯水5 mL常压水化,薄膜完全溶解后,冷却至室温,再进行超声,即得AE-TMP-Lip,所得脂质体呈淡黄色,澄清透明,粒径(146±18)nm,分散指数(PDI)为16.8±3.2。Objective:The objective of this study was to prepare liposome nanoparticles containing aloe emodin and ligustrazine(AE-TMP-LIP),optimize the formulation,and determine the optimal processing conditions for AE-TMP-LIP.Methods:Liposomes were prepared using the film dispersion method.The UV absorbance of AE and TMP was determined using UV spectrophotometry.The prescription and preparation process were optimized using a star design-effect surface method,with investigation factors including solvent selection,solvent dosage,temperature,and other single factors.The drug content in the liposomes was used as an index to verify the results.Results:Among all investigated factors,changes in temperature at 45℃,amount of ultra-pure water used,and amount of film forming solvent had the greatest influence on liposome content.Optimal process optimization conditions were determined through a star design-effect surface method involving three factors at three levels.Conclusion:To prepare AE-TMP-LIP,it is recommended to use 1 mg of aloe emodin and ligustrazine each,along with 30 mg soy lecithin,10 mg cholesterol,13 mg Tween-80.These ingredients were dissolved in trichloromethane methanol organic solvent(4∶1 ratio),followed by ultrasonication.After complete film formation under rotary pressure evaporation at a temperature of 45℃,adjust hydration temperature to 35℃.Once lipid films are completely dissolved and cooled to room temperature,add 5 mL ultra-pure water for atmospheric hydration.The resulting liposomes should be light yellow in color,clear and transparent,with an average particle size of(146±18)nm,and dispersion index(PDI)of 16.8±3.2.

关 键 词：芦荟大黄素 川芎嗪 纳米脂质体 溶解度 制剂优化 

分 类 号：R284.1[医药卫生—中药学]