Page 146 - 《精细化工》2020年 第10期

第 37 卷第 10 期 精 细 化 工 Vol.37, No.10
2020 年 10 月 FINE CHEMICALS Oct. 2020

医药与日化原料
荷叶碱自组装纳米粒的制备与评价

2
1
2
1
1*
2
但 凡 ，姜 维 ，徐彩菊 ，樊洁敏 ，吴平谷 ，蒋益虹
（1. 浙江大学 生物系统工程与食品科学学院，浙江 杭州 310058；2. 浙江省疾病预防控制中心，浙江 杭
州 310051）
摘要：以大豆卵磷脂和壳聚糖为原料，制备磷脂-壳聚糖自组装纳米粒包埋荷叶碱以提高荷叶碱的稳定性，以包
封率为指标探究最佳制备工艺，并对纳米粒的贮藏稳定性、消化稳定性和体外释放特性进行评价。结果表明，
当磷脂与壳聚糖质量比为 20∶1 时，原始的溶剂注入法制备的荷叶碱自组装纳米粒包封率只有 20.08%；在修改
后的溶剂注入法下，在壳聚糖水相中添加质量浓度为 20 g/L 的水溶性维生素 E 时具有最大包封率（51.13%），
此时纳米粒的平均粒径为 142.23 nm，电位为+24.57 mV，外形类似球形。自组装纳米粒可显著提升荷叶碱的贮
藏稳定性和消化稳定性（P<0.05）。室温下（25 ℃）经包埋的荷叶碱的半衰期由未被包埋时的 36.2 d 提升至 53.1 d，
在低温（4 ℃）下经包埋的荷叶碱的半衰期由未被包埋时的 56.2 d 提升至 86.2 d；被纳米粒包埋的荷叶碱经肠
消化后的保留率由未被包埋时的 20.29%提升至 82.98%。体外模拟释放实验表明，自组装纳米粒具有一定的
缓释性。
关键词：荷叶碱；自组装纳米粒；包封率；稳定性；医药原料
中图分类号：TQ460.6 文献标识码：A 文章编号：1003-5214 (2020) 10-2076-08

Preparation and evaluation of self-assembled nanoparticles of nuciferine

2
2
1*
2
1
1
DAN Fan , JIANG Wei , XU Caiju , FAN Jiemin , WU Pinggu , JIANG Yihong
(1. College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, Zhejiang, China;2.
Zhejiang Provincial Center for Disease Control and Prevention, Hangzhou 310051, Zhejiang, China)
Abstract: To improve the stability of nuciferine, nuciferine-encapsulated phospholipid-chitosan
self-assembled nanoparticles were prepared using soybean lecithin and chitosan as raw materials. The
encapsulation efficiency was used as index to explore the optimum preparation process. The storage
stability, digestion stability and in vitro release characteristics of the self-assembled nanoparticles were
evaluated. The results showed that the encapsulation efficiency of nuciferin from the self-assembled
nanoparticles prepared by the original solvent injection method was only 20.08% when the mass ratio of
soybean lecithin to chitosan was 20∶1, while the maximum encapsulation efficiency (51.13%) of
nuciferine from the self-assembled nanoparticles by the modified solvent injection method was obtained
when water-soluble vitamin E with a mass concentration of 20 g/L was added to the aqueous phase of
chitosan. At this time, the nuciferine-encapsulated self-assembled nanoparticles had an average particle size
of 142.23 nm and potential of +24.57 mV, and exhibited similar to a spherical shape. The prepared
self-assembled nanoparticles could significantly improve the storage stability and digestive stability of
nuciferine (P<0.05). The half-life of nuciferine at room temperature (25 ℃) was increased from 36.2 d to
53.1 d, while at low temperature (4 ℃) was increased from 56.2 d to 86.2 d. After gastrointestinal digestion,
the retention rate of nuciferine from the nuciferine-encapsulated self-assembled nanoparticles was 82.98%,
higher than that of nuciferine without encapsulation(20.29%). In vitro simulated release experiments
demonstrated that the nuciferine- encapsulated self-assembled nanoparticles had a certain sustained release.
Key words: nuciferine; self-assembled nanoparticles; encapsulation efficiency; stability; drug materials

收稿日期：2020-04-06; 定用日期：2020-06-09; DOI: 10.13550/j.jxhg.20200297
作者简介：但 凡（1995—），男，硕士生。联系人：蒋益虹（1972—），女，副教授，E-mail：yhjiang6@163.com。