LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Portugal, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Molecules. 2019 Jan 18;24(2):346. doi: 10.3390/molecules24020346.
Polymeric nanoparticles based on fucoidan and chitosan were developed to deliver quercetin as a novel functional food. Through the polyelectrolyte self-assembly method, fucoidan/chitosan (F/C) nanoparticles were obtained with three different weight ratios (1/1, 3/1, and 5/1). The content of quercetin in the fucoidan/chitosan nanoparticles was in the range 110 ± 3 to 335 ± 4 mg·mL, with the increase of weight ratio of fucoidan to chitosan in the nanoparticle. Physicochemically stable nanoparticles were obtained with a particle size within the 300⁻400 nm range and surface potential higher than +30 mV for the 1F/1C ratio nanoparticle and around -30 mV for the 3F/1C and 5F/1C ratios nanoparticles. The 1F/1C ratio nanoparticle became larger and more unstable as the pH increased from 2.5 to 7.4, while the 3F/1C and 5F/1C nanoparticles retained their initial characteristics. This result indicates that the latter nanoparticles were stable along the gastrointestinal tract. The quercetin-loaded fucoidan/chitosan nanoparticles showed strong antioxidant activity and controlled release under simulated gastrointestinal environments (in particular for the 3F/1C and 5F/1C ratios), preventing quercetin degradation and increasing its oral bioavailability.
基于褐藻聚糖和壳聚糖的聚合物纳米粒子被开发出来，以槲皮素作为新型功能性食品进行递送。通过聚电解质自组装方法，得到了三种不同质量比（1/1、3/1 和 5/1）的褐藻聚糖/壳聚糖（F/C）纳米粒子。褐藻聚糖/壳聚糖纳米粒子中槲皮素的含量范围为 110±3 至 335±4mg·mL，随着纳米粒子中褐藻聚糖与壳聚糖的质量比增加而增加。通过物理化学稳定的纳米粒子，粒径在 300⁻400nm 范围内，表面电位对于 1F/1C 比例的纳米粒子高于+30mV，对于 3F/1C 和 5F/1C 比例的纳米粒子约为-30mV。当 pH 值从 2.5 增加到 7.4 时，1F/1C 比例的纳米粒子变得更大且更不稳定，而 3F/1C 和 5F/1C 纳米粒子保持其初始特性。这一结果表明，后者的纳米粒子在整个胃肠道中是稳定的。负载槲皮素的褐藻聚糖/壳聚糖纳米粒子在模拟胃肠道环境下（特别是对于 3F/1C 和 5F/1C 比例）表现出较强的抗氧化活性和控制释放能力，防止了槲皮素的降解并提高了其口服生物利用度。
