Department of Food and Nutrition , Hanyang University , 222 Wangsimni-ro , Seongdong-gu, Seoul 04763 , Republic of Korea.
J Agric Food Chem. 2019 Aug 7;67(31):8609-8616. doi: 10.1021/acs.jafc.9b00008. Epub 2019 Jul 25.
Quercetin (QUE)-loaded nanoparticles (QCG-NPs) were fabricated by ionic gelation between chitosan (CS) and gum arabic (GA) at pH 3.5. At constant CS (0.5 mg/mL) and QUE (60 μM) concentrations, QCG-NPs (260-490 nm) were prepared uniformly with 0.8-2.2 mg/mL GA and exhibited high QUE encapsulation efficiency (94.8-98.0%) and sustained QUE release (4.42-8.89% after 8 h). Because of the electrostatic interaction between QCG-NPs and the mucin layer, in vitro mucin and cell adhesion of QUE were significantly ( < 0.05) enhanced in QCG-NPs (0.44-0.48 mg/mL and 31.7-78.5%), respectively, and the adhesiveness was significantly ( < 0.05) increased with an increase of GA. Because particle size and adhesion properties affect the surface area and retention time of QCG-NPs at the absorption site, cell permeation of QUE through simple diffusion by QCG-NPs exhibited the same tendency as the adhesion results. These data were verified in cellular antioxidant and in vivo ferric reducing abilities of plasma assays that evaluated the antioxidant activities of QUE absorbed into an intestinal cell model and rat blood, respectively. The results provide a better understanding of QCG-NP absorption and indicate that QCG-NPs with mucoadhesion properties can be an effective delivery system for improving QUE absorption.
槲皮素（QUE）负载的纳米粒子（QCG-NPs）是通过壳聚糖（CS）和阿拉伯胶（GA）在 pH 3.5 下的离子凝胶作用制备的。在恒定的 CS（0.5mg/mL）和 QUE（60μM）浓度下，用 0.8-2.2mg/mL 的 GA 均匀制备 QCG-NPs（260-490nm），表现出高 QUE 包封效率（94.8-98.0%）和持续 QUE 释放（8h 后释放 4.42-8.89%）。由于 QCG-NPs 与粘蛋白层之间的静电相互作用，QUE 的体外粘蛋白和细胞黏附显著增加（<0.05）分别为 QCG-NPs（0.44-0.48mg/mL 和 31.7-78.5%），并且随着 GA 的增加，黏附性显著增加（<0.05）。由于粒径和粘附特性影响 QCG-NPs 在吸收部位的表面积和保留时间，通过 QCG-NPs 的简单扩散 QUE 的细胞渗透具有与粘附结果相同的趋势。这些数据在细胞抗氧化和体内血浆还原能力测定中得到了验证，分别评估了 QUE 被吸收到肠细胞模型和大鼠血液中的抗氧化活性。结果提供了对 QCG-NP 吸收的更好理解，并表明具有粘附特性的 QCG-NPs 可以成为提高 QUE 吸收的有效递送系统。
