荷叶碱自组装纳米粒的制备与评价

Preparation and Evaluation of Self-Assembled Nanoparticles of Nuciferine

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来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：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分数为2%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142.23nm，电位为+24.57mV，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）：在室温下（25℃）经包埋的荷叶碱的半衰期由未被包埋时的36.2d提升至53.1d，在低温下（4℃）经包埋的荷叶碱的半衰期由未被包埋时的56.2d提升至86.2d；被纳米粒包埋的荷叶碱经肠胃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。

Abstract:

Phospholipid-chitosan self-assembled nanoparticles were prepared to embed nuciferine to improve its stability. The encapsulation rate was used as the index to explore the best preparation process. At the same time, the storage stability, digestion stability and in vitro release characteristics of the nanoparticles were evaluated. The results showed that under the original solvent injection method, the encapsulation rate was found to be only 20.08%. Using the modified solvent injection method, it was found that the maximum encapsulation rate was 51.13% when the water-soluble vitamin E with a mass fraction of 2% was added to the chitosan aqueous phase. At this time, the average particle size of the nanoparticles was 142.23nm, the potential was + 24.57mV, and the appearance was similar to a spherical shape. Self-assembled nanoparticles can significantly improve the storage stability of nuciferine (p <0.05), and the half-life of nuciferine at room temperature (25 ℃) was increased from 36.2d to 53.1d, and at low temperature (4 ℃) was increased from 56.2d to 86.2d. The self-assembled nanoparticles increased the retention rate of nuciferine after gastrointestinal digestion from 20.29% to 82.98% in the digestion stability experiment, and showed a certain sustained release in the in vitro simulated release experiment.