首页|芦荟大黄素与川芎嗪纳米脂质体的制备及工艺条件优化

芦荟大黄素与川芎嗪纳米脂质体的制备及工艺条件优化

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目的:制备芦荟大黄素-川芎嗪脂质体纳米粒(Aloe emodin-tetramethylpyrazine liposome nanoparticles,AE-TMP-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-80 13 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.
Preparation and optimization of aloe emodin and ligustrazine nanoliposomes
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.

Aloe emodintetramethylpyrazinenanoliposomesolubilityoptimization of formulation

唐佳梅、宋佳文、郭力

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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

芦荟大黄素 川芎嗪 纳米脂质体 溶解度 制剂优化

2025

中药与临床
成都中医药大学

中药与临床

影响因子:0.885
ISSN:1674-926X
年,卷(期):2025.16(1)