高等学校化学学报

高等学校化学学报 ›› 2013, Vol. 34 ›› Issue (1): 236.doi: 10.7503/cjcu20120294

• 高分子化学 • 上一篇    下一篇

可降解聚合物包覆次血红素六肽微球的制备及生物活性

赵天倚1, 赵继鹏1, 雷莉妍1, 陈晓光1, 王立成2, 陈学思3, 王丽萍1   

  1. 1. 吉林大学生命科学学院, 长春 130012;
    2. 吉林大学化学学院, 长春 130012;
    3. 中国科学院长春应用化学研究所, 高分子物理和化学国家重点实验室, 长春 130022
  • 收稿日期:2012-04-01 发布日期:2012-12-31
  • 通讯作者: 王丽萍,女,博士,教授,主要从事药物筛选与设计方面的研究.E-mail:wanglp@jlu.edu.cn E-mail:wanglp@jlu.edu.cn
  • 基金资助:

    吉林省自然科学基金(批准号: 201015171), 吉林省医药产业发展专项(批准号: YYZX201150-2)和吉林省科技发展计划项目(批准号: 201205017)资助.

Preparation and Bioactivities of DhHP-6-loaded Biodegradable Polymeric Microspheres

ZHAO Tian-Yi1, ZHAO Ji-Peng1, LEI Li-Yan1, CHEN Xiao-Guang1, WANG Li-Cheng2, CHEN Xue-Si3, WANG Li-Ping1   

  1. 1. Academy of Life Science, Jilin University, Changchun 130012, China;
    2. College of Chemistry, Jilin University, Changchun 130012, China;
    3. Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
  • Received:2012-04-01 Published:2012-12-31

PDF (PC)

被引次数

20

摘要：

采用水包油包水(W1/O/W2)复乳溶剂挥发法制备了包覆次血红素六肽(DhHP-6)的2种聚酯微球. 通过扫描电子显微镜、 体外缓释行为、 高效液相(HPLC)检测、 酶活力测定和初步的动物实验等表征, 综合评价了载药微球的体外释放及体内生物活性. 实验结果表明, 载药微球球体圆整, 粒径分布均匀, 载药量高, 能够实现体外缓释, 并对细胞过氧化损伤和小鼠脑缺血损伤均有一定的保护作用.

关键词: 载药微球, 次血红素六肽, 聚乙交酯-丙交酯, 聚丙交酯-乙交酯/聚乙二醇, 缓释

Abstract:

Two polyester microspheres were prepared by a water-in-oil-in-water(W1/O/W2) double emulsion solvent evaporation and deuterohaemin-β-AHTVEK(DhHP-6) was encapsulated to the polyester microspheres by a technique with good sphericity and high efficiency. The in vitro release profiles and in vivo biological activity of the polyester microspheres were evaluated by scanning electron microscope(SEM), in vitro release, high performance liquid(HPLC), enzyme activity detection and animal experiments. The data suggested that the drug-loaded polyester microspheres were spherical morphology with narrow size distribution, and had high entrapment capacity with great in vitro release profiles. Furthermore, the drug-loaded polyester microspheres had protective effects on cell injury induced by hydrogen peroxide and cerebral ischemic injury in mice.

Key words: Drug-loaded microsphere, Deuterohaemin-β-AHTVEK(DhHP-6), Polylactic-co-glycolic acid(PLGA), Polylactic-co-glycolic acid/PEG, Sustained-release

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