天然产物研究与开发 ›› 2024, Vol. 36 ›› Issue (9): 1592-1599.doi: 10.16333/j.1001-6880.2024.9.015

• 开发研究 • 上一篇    下一篇

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

胡迪迪1,薛   昊2,金旭东1,李宛俞1,徐湘迪1,陈   靖1,3*   

  1. 1扬州大学医学院(转化医学研究院),扬州225001;2深圳大学医学部生物医学工程学院,深圳 518000;3江苏省中西医结合老年病防治重点实验室,扬州225001
  • 出版日期:2024-09-25 发布日期:2024-09-25
  • 基金资助:
    宁夏自然科学基金(2023AAC03679)

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

HU Di-di1,XUE Hao2,JIN Xu-dong3,LI Wan-yu1,XU Xiang-di1,CHEN Jing1,3*   

  1. 1School of Medicine(Institute of Translational Medicine),Yangzhou University,Yangzhou 225001,China;2School of Biomedical Engineering,Medical School,Shenzhen University,Shenzhen 518000,China;3Jiangsu Key Laboratory of Integrated Traditional Chinese  adn Western Medicine for Prevention and Treatment of Senile Diseases,Yangzhou 225001,China
  • Online:2024-09-25 Published:2024-09-25

摘要:

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。

关键词: 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

Abstract:

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,water-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 optimal 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,therefore,is stable,reproducible and feasible,and the prepared nanoparticles possess a satisfying solution stability.

Key words:

中图分类号:  R943