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活性氧响应的白及多糖载药胶束制备及其表征
引用本文:党婷婷,王济,唐鹏,王晓娟.活性氧响应的白及多糖载药胶束制备及其表征[J].中草药,2018,49(23):5548-5553.
作者姓名:党婷婷  王济  唐鹏  王晓娟
作者单位:陕西中医药大学, 陕西 咸阳 712046;军事口腔医学国家重点实验室, 口腔疾病国家临床医学研究中心, 陕西省口腔生物工程技术研究中心, 第四军医大学口腔医院药剂科, 陕西 西安 710032,军事口腔医学国家重点实验室, 口腔疾病国家临床医学研究中心, 陕西省口腔生物工程技术研究中心, 第四军医大学口腔医院药剂科, 陕西 西安 710032,西安交通大学生命科学与技术学院, 生物医学信息工程教育部重点实验室, 陕西 西安 710049,军事口腔医学国家重点实验室, 口腔疾病国家临床医学研究中心, 陕西省口腔生物工程技术研究中心, 第四军医大学口腔医院药剂科, 陕西 西安 710032
摘    要:目的制备活性氧响应的白及多糖载药胶束,进行处方、制备工艺优化,并进行体外评价。方法合成活性氧响应白及多糖载体材料,以姜黄素为模型药物,采用透析法制备载药胶束;通过单因素和正交设计法优化处方;用透射电镜和激光粒子测定仪对胶束的形态和粒径分布、Zeta电位进行表征;用过氧化氢模拟活性氧环境,观察胶束形态变化。结果在优化条件下制备的载药胶束外观呈圆球形,分布均匀,平均粒径为(225.33±2.97)nm,Zeta电位为(-16.80±0.37)m V,包封率为(85.75±0.87)%,载药量为(20.21±0.44)%;在氧化条件下胶束材料可发生降解。结论优化条件下制备的白及多糖载药胶束粒径分布均匀,包封率和载药量良好。

关 键 词:活性氧响应  白及多糖  姜黄素  胶束  处方优化  体外评价
收稿时间:2018/7/16 0:00:00

Preparation and characterization of reactive oxygen species-responsive Bletilla striata polysaccharide micelle
DANG Ting-ting,WANG Ji,TANG Peng and WANG Xiao-juan.Preparation and characterization of reactive oxygen species-responsive Bletilla striata polysaccharide micelle[J].Chinese Traditional and Herbal Drugs,2018,49(23):5548-5553.
Authors:DANG Ting-ting  WANG Ji  TANG Peng and WANG Xiao-juan
Institution:Shaanxi University of Chinese Medicine, Xianyang 712046, China;State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, Hospital of Stomatology, The Fourth Military Medical University, Xi''an 710032, China,State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, Hospital of Stomatology, The Fourth Military Medical University, Xi''an 710032, China,Key Laboratory of Biomedicine Information Engineering of Education Ministry, School of Life Sciense and Technology, Xi''an Jiaotong University, Xi''an 710049, China and State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, Hospital of Stomatology, The Fourth Military Medical University, Xi''an 710032, China
Abstract:Objective To prepare reactive oxygen species (ROS)-responsive Bletilla striata polysaccharide (Oxi-BSP) micelles, optimize their preparation technnology, and evaluate its in vitro characterizations. Methods Oxi-BSP was synthesized, then curcumin (Cur)-loaded micelles were prepared by a dialysis method. The formulation and preparation technology was optimized using an orthogonal design method. The morphology was observed by transmission electron microscope, while the particle size, particle distribution, and zeta potential were determined by laser particle size analyzer. Hydrogen peroxide was used to simulate the ROS environment and then the change of micellar morphology was observed. Results The Cur-loaded micelles were spherical with homogeneous distribution, the mean size was (225.33 ±2.97) nm, the zeta potential was (-16.80 ±0.37) mV, the encapsulation efficiencies was (85.75 ±0.87)%, and drug loading capacities was (20.21 ±0.44)%. And the micelles were responsive to ROS stimuli. Conclusion The obtained micelles display an uniform particle size distribution with moderate drug encapsulation efficiencies and drug loading capacities.
Keywords:reactive oxygen species  Bletilla striata polysaccharide  curcumin  micelles  formulation optimization  in vitro evaluation
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