| 季铵化壳聚糖胰岛素纳米粒的制备、处方优化及其初步药效学实验 |
| 投稿时间：2015-02-10 修订日期：2015-06-02 点此下载全文 |
| 引用本文：苑旺,王美玲,石岩,崔黎丽.季铵化壳聚糖胰岛素纳米粒的制备、处方优化及其初步药效学实验[J].药学实践杂志,2015,33(4):319~323 |
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| 基金项目:国家自然科学基金(No.51477175) |
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| 中文摘要:目的 采用正交设计试验优化载胰岛素季铵化壳聚糖纳米粒的处方工艺,并初步考察其降糖效果。 方法 用离子交联法制备载胰岛素的季铵化壳聚糖纳米粒,用正交试验确定其最佳处方工艺。用透射电子显微镜观察纳米粒的表面形态;用粒径/Zeta电位仪测定纳米粒的粒径和Zeta电位;用高效液相色谱(HPLC)法测定纳米粒的包封率、载药量及体外释放情况。对糖尿病大鼠皮下注射给药,对其药效学进行初步考察。 结果 制得的纳米粒呈球形,分布均匀;平均粒径(63.26±1.88) nm;Zeta电位(33.1±0.3) mV;包封率(37.92±2.11)%;载药量(5.42±0.3)%;24 h累计释放率63.83%。皮下注射给药8 h,糖尿病大鼠血糖较单纯注射胰岛素组下降平缓,且药效持久。 结论 优化后的载胰岛素的季铵化壳聚糖纳米粒形态较好、粒径较小,为研究胰岛素的新型给药途径奠定了基础。 |
| 中文关键词:胰岛素 纳米粒 离子交联法 正交设计 |
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| Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles |
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| Abstract:Objective To prepare and optimize insulin-loaded N-trimethyl chitosan nanoparticles via orthogonal design, and preliminarily study the effects on blood glucose level. Methods The insulin-loaded N-trimethyl chitosan nanoparticles(INS-NPs) were prepared by ionic gelation, and the optimal proportion was obtained with orthogonal design. The nanoparticles were characterized by transmission electron microscopy and zeta/sizer nano analyzer. The entrapment efficiency of insulin-loaded nanoparticles and the in vitro releasing characteristics were studied by HPLC. A preliminary pharmacodynamic study of the insulin-loaded nanoparticles was also carried out. Results The INS-NPs exhibited narrow distribution. The mean diameter of INS-NPs was (63.26±1.88)nm, while the entrapment efficiency was (37.92±2.11)%. After 8 hours of subcutaneous injection of the INS-NPs, the blood glucose level in diabetic rats decreased to normal level and kept stable. Conclusion The optimized insulin-loaded nanoparticles had homogeneous spherical shape, small size, and could be a new approach of administration for insulin. |
| keywords:insulin nanoparticles ionic gelation orthogonal design |
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