穿心莲内酯甲氧基聚乙二醇-聚乳酸-羟基乙酸纳米粒处方优化及体外释药考察  

Formulation optimization of andrographolide mPEG-PLGA nanoparticles and in vitro release study

作　　者：卢慧芳[1] 刘艳美[1] 王荷香[1] 周敏[1] 李晓婷 郝海军 LU Hui-fang;LIU Yan-mei;WANG He-xiang;ZHOU Min;LI Xiao-ting;HAO Hai-jun(College of Animal Husbandry Engineering,Henan Agricultural Vocational College,Henan Zhengzhou 451450,China;Department of Pharmaceutical Engineering,Zhengzhou University of Industrial Technology,Henan Zhengzhou 451150,China;Department of Pharmacy,Shanghai Institute of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]河南农业职业学院牧业工程学院,河南郑州451450 [2]郑州工业应用技术学院制药工程系,河南郑州451150 [3]上海市中药研究所药学部,上海201203

出　　处：《中国医院药学杂志》2022年第19期2034-2039,共6页Chinese Journal of Hospital Pharmacy

摘　　要：目的:优化穿心莲内酯甲氧基聚乙二醇-聚乳酸-羟基乙酸[methoxy poly(ethylene glycol)-poly(lactic-co-glycolic acid),mPEG-PLGA]纳米粒处方,并进行体外释药评价。方法:乳化法制备穿心莲内酯mPEG-PLGA纳米粒,Box-Behnken设计-效应面法筛选穿心莲内酯mPEG-PLGA纳米粒最优处方,测定包封率、载药量、粒径及Zeta电位。采用质量分数为5%的甘露醇和乳糖等量混合物作为冻干保护剂,进一步制备成冻干粉,考察体外释药行为。结果:穿心莲内酯mPEG-PLGA纳米粒最佳处方为:mPEG-PLGA用量为589 mg、水相体积为70 mL、聚乙二醇硬脂酸酯15(Solutol HS 15)质量分数为1.2%,包封率为(82.07±1.62)%,载药量为(3.87±0.21)%,粒径为(179.56±9.19)nm,Zeta电位为(-10.91±1.84)mV。穿心莲内酯mPEG-PLGA纳米粒体外释药具有缓释特征,释药过程符合Weibull模型:lnln[1/(1-M_(t)/M_(∞))]=0.4103lnt-1.4341。结论:可用Box-Behnken设计-效应面法优化穿心莲内酯mPEG-PLGA纳米粒,为后续研究奠定基础。OBJECTIVE To optimize the formulation of andrographolide mPEG-PLGA nanoparticles,and carry out in vitro drug release evaluation.METHODS Emulsification method was employed to prepare andrographolide mPEG-PLGA nanoparticles.Box-Behnken response surface design method was used to investigate the optimal formulation of andrographolide mPEG-PLGA nanoparticles.Entrapment efficiency,drug loading,particle size and Zeta potential were determined.A mixture of mannitol and lactose with a mass fraction of 5%was used as freeze-drying protectant,lyophilized powder was prepared and the release behavior in vitro was investigated.RESULTS The optimal formulation of andrographolide mPEG-PLGA nanoparticles was as follows:mPEG-PLGA dosage was 589 mg,water phase volume was 70 mL and Solutol HS 15 quality score was 1.2%.The envelopment efficiency,drug loading,particle size and Zeta potential were(82.07±1.62)%,(3.87±0.21)%,(179.56±9.19)nm and(-10.91±1.84)mV,respectively.The drug release in vitro showed obvious sustained-release characteristics,and the release process conformed to the following Weibull model:lnln[1/(1-M_(t)/M_(∞))]=0.4103lnt-1.4341.CONCLUSION Box-Behnken design-response surface method can be employed to optimize formulation of andrographolide mPEG-PLGA nanoparticles,which lays foundation for the further studies.

关 键 词：穿心莲内酯 mPEG-PLGA纳米粒 冻干粉 Weibull模型 

分 类 号：R943[医药卫生—药剂学]