首页|单因素结合Box-Benhnken响应曲面法优化载青蒿素聚乳酸-羟基乙酸共聚物纳米粒制备工艺

单因素结合Box-Benhnken响应曲面法优化载青蒿素聚乳酸-羟基乙酸共聚物纳米粒制备工艺

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本研究优化包载青蒿素(artemisinin,ART)聚乳酸-羟基乙酸共聚物(poly(lactic-co-glycolic acid),PLGA)纳米粒(PLGA-ART-NPs)的最优工艺.首先采用乳化-溶剂法制备纳米粒,以单因素实验确定乳化剂种类(聚乙烯醇、吐温80、泊洛沙姆)、乳化剂浓度、水-油两相比例及载体-药物比例对粒径、载药量、包封率的影响;以载药量为评价指标,通过Box-Benhnken响应面法,进一步优化PLGA-ART-NPs制备工艺.结果表明聚乙烯醇乳化效果最好,以乳化剂浓度、水-油两相比例、载体-药物比例为影响因素,最优处方确定为:乳化剂浓度为0.017 g/mL,水-油两相比例为18∶1(V/V),载体-药物比例为10∶1(W/W).以最优处方制备的纳米粒载药量为(4.43±0.22)%,zeta电位为-28.28±2.17 mV,表明本文优化后的处方工艺条件稳定,重复性良好,可行性高,制得的纳米溶液稳定性良好.
Optimization of the preparation technics of artemisinin-loaded lactic-co-glycolic acid nanoparticles based on Box-Benhnken response surface method combined with a single factor analysis
This study aims to optimize the preparation technics of artemisinin(ART)loaded lactic-co-glycolic acid(PLGA)nanoparticles(PLGA-ART-NPs).The emulsification-solvent evaporation method was performed to prepare the nanoparticles.The influnences of emulisifier types(polyvinyl alcohol,Tween 80,and poloxamer),the concentrations of the emulisifier,wa-ter-oil ratio,and carrier-drug ratio on the particle size,encapsulation efficiency,and drug loading capacity were analyzed by a single factor analysis.The preparation technics of PLGA-ART-NPs were optimized by using drug loading capacity as the index based on a Box-Benhnken response surface method.The results indicated that polyvinyl alcohol had a better emulsification effect.Emulsifier concentration,water-oil phase ratio,and carrier-drug ratio were chosen as the influence factors and the opti-mal formulations were as follows:emulsifier concentration of 0.017 g/mL,water-oil phase ratio of 18∶1(V/V),and carrier-drug ratio of 10∶1(W/W).Drug loading rate for the nanoparticles prepared under the optimal conditions was detected to be(4.43±0.22)%together with zeta potential at-28.28±2.17 mV.The formulation process optimized in this work,there-fore,is stable,reproducible and feasible,and the prepared nanoparticles possess a satisfying solution stability.

polylactic acid-glycolic acid copolymerartemisinin nanoparticlesresponse surface methodsingle factor analysisemulsification-solvent evaporation method

胡迪迪、薛昊、金旭东、李宛俞、徐湘迪、陈靖

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扬州大学医学院(转化医学研究院),扬州 225001

深圳大学医学部生物医学工程学院,深圳 518000

江苏省中西医结合老年病防治重点实验室,扬州 225001

聚乳酸-羟基乙酸共聚物 青蒿素纳米粒 响应曲面法 单因素分析 乳化-溶剂挥发法

宁夏自然科学基金

2023AAC03679

2024

天然产物研究与开发
中国科学院成都文献情报中心

天然产物研究与开发

CSTPCD北大核心
影响因子:0.783
ISSN:1001-6880
年,卷(期):2024.36(9)
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