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木香烃内酯与去氢木香内酯共包封聚乙二醇化长循环脂质体的制备及表征
引用本文:王文俊,严晓敏,陈自强,李奇娟,谢余,胡慧玲,王战国. 木香烃内酯与去氢木香内酯共包封聚乙二醇化长循环脂质体的制备及表征[J]. 中草药, 2019, 50(17): 4068-4075
作者姓名:王文俊  严晓敏  陈自强  李奇娟  谢余  胡慧玲  王战国
作者单位:成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都中医药大学药学院, 中药材标准化教育部重点实验室, 西南特色中药资源国家重点实验室培育基地, 四川 成都 611137,成都大学医学院, 代谢组学协同创新实验室, 羌医药标准研究推广基地暨协同创新中心, 四川 成都 610106
基金项目:成都中医药大学杏林学者项目(QNXZ2018010);成都中医药大学校基金项目(XYPY1505)
摘    要:目的优化川木香主要药效成分木香烃内酯(Cos)与去氢木香内酯(DL)共包封的聚乙二醇(PEG)化长循环脂质体的制备工艺,并对其进行表征。方法采用薄膜水化法制备Cos与DL共包封的PEG化长循环脂质体,以包封率为指标,通过单因素考察结合Box-Behnken响应面法对处方进行优化,并对脂质体的形态、粒径及表面电位、包封率、稳定性和体外释放度进行测定。结果最佳制备工艺为药脂比0.14∶1、胆固醇与磷脂比0.05∶1、m PEG-2000-DSPE添加量6%、水化时间30 min、探头超声时间4 min。所得脂质体外观圆整、分散均匀,平均粒径为(104.80±2.48)nm,多分散指数(PDI)为0.245±0.031,Zeta电位(-9.70±0.23)m V,Cos包封率(91.9±2.6)%,DL的包封率(94.41±1.23)%。结论工艺和处方优化后制得外观形态良好、配伍药物包封率均较高的PEG化脂质体。

关 键 词:木香烃内酯  去氢木香内酯  PEG  长循环脂质体  薄膜水化法  包封率  单因素实验  Box-Behnken响应面法  稳定性  体外释放度
收稿时间:2019-08-12

Preparation and characterization of PEGylated long-circulating liposomes encapsulating costunolide and dehydrocostus lactone
WANG Wen-jun,YAN Xiao-min,CHEN Zi-qiang,LI Qi-juan,XIE Yu,HU Hui-ling and WANG Zhan-guo. Preparation and characterization of PEGylated long-circulating liposomes encapsulating costunolide and dehydrocostus lactone[J]. Chinese Traditional and Herbal Drugs, 2019, 50(17): 4068-4075
Authors:WANG Wen-jun  YAN Xiao-min  CHEN Zi-qiang  LI Qi-juan  XIE Yu  HU Hui-ling  WANG Zhan-guo
Affiliation:Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China and Collaborative Innovation Laboratory of Metabonomics, Standard Research and Extension Base & Collaborative Innovation Center of Qiang Medicine, School of Medicine, Chengdu University, Chengdu 610106, China
Abstract:
Keywords:costunolide  dehydrocostus lactone  PEG  long-circulating liposomes  thin film hydration method  encapsulation efficiency  single-factor experiment  Box-Behnken response surface method  stability  in vitro release
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