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

苑旺; 王美玲; 石岩; 崔黎丽

doi:10.3969/j.issn.1006-0111.2015.04.008

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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

苑旺, 王美玲, 石岩, 崔黎丽

文章导航 > 药学实践与服务 > 2015 > 33(4): 319-323

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]. 药学实践与服务, 2015, 33(4): 319-323. doi: 10.3969/j.issn.1006-0111.2015.04.008

引用本文:

YUAN Wang, WANG Meiling, SHI Yan, CUI Lili. Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 319-323. doi: 10.3969/j.issn.1006-0111.2015.04.008

Citation:

YUAN Wang, WANG Meiling, SHI Yan, CUI Lili. Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 319-323. doi: 10.3969/j.issn.1006-0111.2015.04.008

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

doi: 10.3969/j.issn.1006-0111.2015.04.008

1.
第二军医大学药学院无机化学教研室, 上海 200433
2.
第二军医大学基础部数理教研室, 上海 200433
3.
第二军医大学海军医学系, 上海 200433

基金项目: 国家自然科学基金(No.51477175)

Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles

1.
Department of Inorganic Chemistry, School of Pharmacy; Second Military Medical University, Shanghai 200433, China
2.
Department of Physics and Mathematics, College of Basic Medical Sciences; Second Military Medical University, Shanghai 200433, China
3.
College of Naval Medicine, Second Military Medical University, Shanghai 200433, China

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。
- 胰岛素 /
- 纳米粒 /
- 离子交联法 /
- 正交设计
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.
- insulin /
- nanoparticles /
- ionic gelation /
- orthogonal design

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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

doi: 10.3969/j.issn.1006-0111.2015.04.008

1. 第二军医大学药学院无机化学教研室, 上海 200433

2. 第二军医大学基础部数理教研室, 上海 200433

3. 第二军医大学海军医学系, 上海 200433

基金项目: 国家自然科学基金(No.51477175)

收稿日期: 2015-02-10
修回日期: 2015-06-02

关键词:

胰岛素 /

纳米粒 /

离子交联法 /

正交设计

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。

English Abstract

Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles

1. Department of Inorganic Chemistry, School of Pharmacy; Second Military Medical University, Shanghai 200433, China

2. Department of Physics and Mathematics, College of Basic Medical Sciences; Second Military Medical University, Shanghai 200433, China

3. College of Naval Medicine, Second Military Medical University, Shanghai 200433, China

Received Date: 2015-02-10
Rev Recd Date: 2015-06-02

Keywords:

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.

引用本文:

Citation:

YUAN Wang, WANG Meiling, SHI Yan, CUI Lili. Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 319-323. doi: 10.3969/j.issn.1006-0111.2015.04.008

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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

doi: 10.3969/j.issn.1006-0111.2015.04.008

Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles

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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

doi: 10.3969/j.issn.1006-0111.2015.04.008

1. 第二军医大学 药学院无机化学教研室, 上海 200433 2. 第二军医大学 基础部数理教研室, 上海 200433 3. 第二军医大学 海军医学系, 上海 200433

English Abstract

Preparation,formulation optimization and preliminary pharmacodynamic experiment of insulin-loaded N-trimethyl chitosan nanoparticles

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目录

1. 第二军医大学药学院无机化学教研室, 上海 200433

2. 第二军医大学基础部数理教研室, 上海 200433

3. 第二军医大学海军医学系, 上海 200433