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

留言板

尊敬的读者、作者、审稿人, 关于本刊的投稿、审稿、编辑和出版的任何问题, 您可以本页添加留言。我们将尽快给您答复。谢谢您的支持!

姓名
邮箱
手机号码
标题
留言内容
验证码

x 关闭永久关闭

《药学实践与服务》杂志目前不收取审稿费、版面费、加急费等费用，如收到邮件声称是编辑部X编辑，要求加作者微信的，请谨防财产损失！编辑部用于作者校对时绑定微信的邮件通过yxsjzzs@163.com发送，标题是《药学实践与服务》XML数字出版服务微信绑定，请区分开。

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

[1]	Unwin N, Gan D, Whiting D. The IDF diabetes atlas: providing evidence, raising awareness and promoting action [J]. Diabetes Res Clin Pract, 2010, 87(1): 2-3.
[2]	韩丽娜,尹丽芳,赵月芳,等.胰岛素/维生素B₁₂-透明质酸纳米粒的制备及口服给药体内外性质的评价[J].中山大学学报,2012,33(5): 597-602.
[3]	欧歌,廖德华,张凯,等.采用离子交联法制备壳聚糖胰岛素纳米粒的研究进展[J].中南药学,2013,11(2): 111-119.
[4]	Avadi MR, Sadeghi AM, Mohammadpour N, et al. Preparation and characterization of insulin nanoparticles using chitosan and arabic gum with ionic gelation method[J]. Nanomedicine, 2010, 6(1): 58-63.
[5]	曹姗,胡凯莉,刘梅,等.多西紫杉醇口服磷脂纳米粒的制备与处方优化[J].中成药,2013, 35(9): 1896-1900.

[1]	赵全公, 王国坤, 徐志云. 虾青素通过激活Nrf2/HO-1通路抑制瓣膜间质细胞钙化 . 药学实践与服务, 2025, 43(): 1-5. doi: 10.12206/j.issn.2097-2024.202412057
[2]	竺东杰, 贺新征, 邹杰, 余史丹, 李红霞. 雷公藤甲素对大鼠脑缺血再灌注损伤的影响及机制研究 . 药学实践与服务, 2025, 43(): 1-6. doi: 10.12206/j.issn.2097-2024.202311021
[3]	吴海韵, 杨甜, 张弛, 梁文仪, 苏娟. 气相色谱-离子迁移谱技术在中药研究中的应用进展 . 药学实践与服务, 2025, 43(): 1-6. doi: 10.12206/j.issn.2097-2024.202409007
[4]	姚小静, 计佩影, 陆峰, 施国荣, 傅翔. 表面增强拉曼光谱法快速测定尿液中曲马多的研究 . 药学实践与服务, 2025, 43(4): 185-189. doi: 10.12206/j.issn.2097-2024.202401072
[5]	肖农, 陆诗依, 唐文雅, 居敏俐, 徐刚锋, 杨明华. 中成药微生物计数法前处理的影响因素和优化方法 . 药学实践与服务, 2025, 43(): 1-5. doi: 10.12206/j.issn.2097-2024.202403014
[6]	魏莱, 董国强, 盛春泉. 靶向SARS-CoV-2主蛋白酶的PROTAC设计、合成与蛋白降解活性研究 . 药学实践与服务, 2025, 43(): 1-8. doi: 10.12206/j.issn.2097-2024.202503063
[7]	施乔, 韩贵焱, 张俊腾, 刘娜. 新型Hsp90抑制剂的设计合成及其抗真菌和抗肿瘤活性研究 . 药学实践与服务, 2025, 43(3): 124-135. doi: 10.12206/j.issn.2097-2024.202501019
[8]	卢熠菲, 宋佳, 沈红霞, 赵庆杰. 新型苦参碱衍生物的设计合成与体外抗炎活性研究 . 药学实践与服务, 2025, 43(): 1-8. doi: 10.12206/j.issn.2097-2024.202503005
[9]	吴若南, 叶爽, 李墨晨轩, 缪震元, 罗川. 冬凌草甲素磺酰脲衍生物的设计与抗炎活性的研究 . 药学实践与服务, 2025, 43(): 1-5. doi: 10.12206/j.issn.2097-2024.202401048
[10]	郭灵怡, 刘艳超, 高路, 刘瑞瑶, 吕权真, 俞媛. 醋酸卡泊芬净单硬脂酸甘油酯纳米粒抗白色念珠菌感染的增效作用研究 . 药学实践与服务, 2025, 43(3): 136-142, 150. doi: 10.12206/j.issn.2097-2024.202310043
[11]	杨贺英, 罗彩萍, 彭婷, 梁文仪, 沈颂章, 苏娟. 花椒生物碱富集纯化工艺优化及其成分分析 . 药学实践与服务, 2025, 43(2): 75-81. doi: 10.12206/j.issn.2097-2024.202404066
[12]	张艺昕, 关欣怡, 王博宁, 闻俊, 洪战英. 二氢吡啶类钙离子拮抗药物手性分析及其立体选择性药动学研究进展 . 药学实践与服务, 2024, 42(8): 319-324. doi: 10.12206/j.issn.2097-2024.202308062
[13]	王晓飞, 张颖, 顾佳钰, 胡馨儿, 张海, 曹岩. 表面等离子共振传感器的识别元件在医药领域中的研究应用进展 . 药学实践与服务, 2024, 42(): 1-9. doi: 10.12206/j.issn.2097-2024.202309014
[14]	王耀振, 徐灿, 吕顺莉, 田泾, 张东炜. 钾离子竞争性酸阻滞剂的药学特征研究进展 . 药学实践与服务, 2024, 42(7): 278-284. doi: 10.12206/j.issn.2097-2024.202306040
[15]	邹思, 吴岩斌, 吴锦忠, 吴建国, 黄家兴. 虎奶菇菌核多糖功能化纳米硒抗疲劳功效研究 . 药学实践与服务, 2024, 42(10): 426-432. doi: 10.12206/j.issn.2097-2024.202206072
[16]	凯丽比努尔·奥布力艾散, 李倩, 谢志, 贾文彦, 尹东锋. 星点设计-效应面法优化仑伐替尼混合胶束的制备工艺 . 药学实践与服务, 2024, 42(11): 495-502. doi: 10.12206/j.issn.2097-2024.202403019

点击查看大图

计量

文章访问数: 3851
HTML全文浏览量: 253
PDF下载量: 758
被引次数: 0

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

全文HTML

参考文献 (5)

下载: 全尺寸图片幻灯片

返回文章

用微信扫码二维码

分享至好友和朋友圈

主管、主办: 中国人民解放军海军军医大学地址: 上海市杨浦区国和路325号邮政编码: 200433

电话: （021）81871324,81871397 E-mail: yxsjzzs@163.com

网站备案号沪ICP备05003363号-1

本系统由北京仁和汇智信息技术有限公司开发

留言板

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

计量

出版历程

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

全文HTML

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