魏颖慧1,赵燕敏1,李 静1, 2,徐小玉1,郭曼曼1,李范珠1.壳聚糖修饰雷公藤多苷纳米粒的制备及其体外释药研究[J].中草药,2013,44():
壳聚糖修饰雷公藤多苷纳米粒的制备及其体外释药研究
Preparation and in vitro release of tripterygium glycosides-loaded nanoparticles modified with chitosan
  
DOI:
中文关键词:  关键词:雷公藤多苷  壳聚糖修饰  纳米粒  正交试验设计  体外释药  自乳化溶剂扩散法
英文关键词:Key words: tripterygium glycosides  chitosan-modified  nanoparticles  orthogonal design  in vitro release  self-emulsifying solvent diffusion method
基金项目:基金项目:国家自然科学基金资助项目(30902007);浙江省重点科技创新团队资助项目(2012R10044-05)
作者单位
魏颖慧1,赵燕敏1,李 静1, 2,徐小玉1,郭曼曼1,李范珠1 1. 浙江中医药大学浙江 杭州 310053 2. 贵州大学贵州 贵阳 550025 
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中文摘要:
      摘 要:目的 制备壳聚糖修饰雷公藤多苷纳米粒(LMWC-TG-NPs),并研究其体外释药行为。方法 采用改良的自乳化 溶剂扩散法制备LMWC-TG-NPs;正交试验设计优化TG-NPs 处方,单因素试验考察LMWC 修饰方式;以含20%乙醇的PBS (pH 7.4)为释放介质考察LMWC-TG-NPs 的体外释药行为。结果 优化的处方工艺:以1.0% Poloxamer 188、80 mg PLA、 12 mL 有机相、丙酮-乙醇(2∶3)制备TG-NPs 混悬液,以与TG-NPs 混悬液等体积的10% LMWC 溶液修饰TG-NPs 制备 LMWC-TG-NPs;根据优化条件制备的LMWC-TG-NPs,外观呈圆形或类圆形,平均粒径为(207.6±3.4)nm,多分散指数 (PDI)为0.078±0.009(n=3),包封率和载药量分别为(61.83±2.43)%、(10.70±0.37)%(n=3);体外释药符合Higuchi 方程。结论 所制备的LMWC-TG-NPs 包封率较高,粒径小,体外释药具有明显的缓释特征,为后期研究其肾脏靶向和毒 性奠定了基础。
英文摘要:
      Abstract: Objective To prepare tripterygium glycosides-loaded nanoparticles modified with 50% N-acetylated low molecular weight chitosan (LMWC) and to investigate their in vitro release behavior. Methods The nanoparticles were prepared by modified self-emulsifying solvent diffusion method (M-SESD) based on the formulation of TG-NPs, which was optimized by orthogonal design, and the modified condition of LMWC, based on the single factor anlysis. The optimized LMWC-TG-NPs systems were characterized by particle size, entrapment efficiency, drug loading and in vitro release. Results The optimized formulation of TG-NPs consists of 1.0% Poloxamer 188, 80 mg PLA, 12 mL oil phase, in which the ratio between acetone and ethanol is determined as 2∶3. The LMWC-TG-NPs are prepared by incubating TG-NPs suspensions with 10% LMWC solution at the ratio of 1∶1. The shape of the prepared tripterygium glycosides-loaded nanoparticles was spherical. The mean particle size, polydispersity index, entrapment efficiency and drug loading were (207.6 ± 3.4) nm, 0.078 ± 0.009, (61.83 ± 2.43)% and (10.70 ± 0.37)% (n=3), respectively. The in vitro release characteristics of LMWC-TG-NPs conform to Higuchi equation in PBS buffer composed of 20% ethanol at pH 7.4. Conclusion The prepared nanoparticles showed a sustained-release characteristics with well-distributed particle size as well as high entrapment efficiency and drug loading.
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