Liu Xiaofeng, Yu Shuzhen, Lu Xiaoqin, Zhang Yao, Zhong Hao, Zhou Zhiyuan, Guan Rongfa
College of Food Science and Technology, Zhejiang University of Technology, Hangzhou, Zhejiang 310014, China.
Zhejiang Provincial Key Lab for Chem and Bio Processing Technology of Farm Produces, School of Biological and Chemical Engineering, Zhejiang University of Science and Technology, Hangzhou, Zhejiang 310023, China.
ACS Omega. 2024 Apr 3;9(15):17154-17162. doi: 10.1021/acsomega.3c09892. eCollection 2024 Apr 16.
Quercetin is a flavonol compound with excellent biological activities. However, quercetin exhibits poor stability and solubility in water, which limits its application. In this study, quercetin nanoliposomes (QUE-NL-1) were prepared using an ultrasonic thin-film dispersion method, and the preparation conditions were optimized using response surface methodology. The optimal conditions for preparing QUE-NL-1 were as follows: an evaporation temperature of 35 °C, a drug concentration of 0.20 mg/mL, and a lipid bile ratio of 4:1. The encapsulation rate of QUE-NL-1 is (63.73 ± 2.09)%, the average particle size is 134.11 nm, and the average absolute value of the zeta potential is 37.50 and PDI = 0.24. By analyzing the storage temperature, storage time, and leakage rate of QUE-NL-1 in simulated gastrointestinal fluid, it was found that quercetin exhibits good stability after embedding and can achieve sustained release in intestinal juice. In addition, the cytotoxicity of QUE-NL-1 was not significant, and the survival rate of Caco-2 cells was >90% when the concentration range of QUE-NL-1 was 0.1-0.4 mg/mL. This study provides an efficient method for preparing QUE-NL-1 with small particle sizes, good stability, and high safety, which is of great significance for expanding the application range of quercetin.
槲皮素是一种具有优异生物活性的黄酮醇化合物。然而，槲皮素在水中表现出较差的稳定性和溶解性，这限制了其应用。在本研究中，采用超声薄膜分散法制备了槲皮素纳米脂质体（QUE-NL-1），并使用响应面法对制备条件进行了优化。制备QUE-NL-1的最佳条件如下：蒸发温度为35℃，药物浓度为0.20mg/mL，脂质与胆汁比例为4:1。QUE-NL-1的包封率为（63.73±2.09）%，平均粒径为134.11nm，ζ电位的平均绝对值为37.50，PDI=0.24。通过分析QUE-NL-1在模拟胃肠液中的储存温度、储存时间和泄漏率，发现槲皮素包封后具有良好的稳定性，并且在肠液中能够实现缓释。此外，QUE-NL-1的细胞毒性不显著，当QUE-NL-1的浓度范围为0.1-0.4mg/mL时，Caco-2细胞的存活率>90%。本研究提供了一种制备粒径小、稳定性好、安全性高的QUE-NL-1的有效方法，这对于扩大槲皮素的应用范围具有重要意义。
