Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats.
Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats.
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DOI：
10.2147/ijn.s68526
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发表时间：
2014
影响因子：
8
通讯作者：
Gálvez J
中科院分区：
文献类型：
--
作者：
Lozano-Pérez AA;Rodriguez-Nogales A;Ortiz-Cullera V;Algieri F;Garrido-Mesa J;Zorrilla P;Rodriguez-Cabezas ME;Garrido-Mesa N;Utrilla MP;De Matteis L;de la Fuente JM;Cenis JL;Gálvez J
我们的目的是评估丝素蛋白纳米颗粒的肠道抗炎特性，约100 nm的大小，当加载芪化合物白藜芦醇，在大鼠结肠炎的实验模型。通过吸附法将白藜芦醇负载到纳米粒上。在RAW 264.7细胞（小鼠巨噬细胞）的细胞培养物中体外测试白藜芦醇负载的纳米颗粒的生物学效应，并且在结肠内给药时在大鼠结肠炎的三硝基苯磺酸模型中体内测试白藜芦醇负载的纳米颗粒的生物学效应。白藜芦醇在1×磷酸盐缓冲盐水（PBS; pH 7.4）中的释放特征在于快速释放，在3小时内达到溶解度极限，其维持超过80小时。体外试验显示，这些白藜芦醇负载的纳米颗粒发挥免疫调节特性，因为它们促进巨噬细胞的活动在基础条件下，并抑制这种活动时，刺激脂多糖。体内实验表明，在对宏观症状、炎症标志物和肠屏障功能进行评估后，负载白藜芦醇的丝素纳米颗粒具有比单一治疗更好的效果，与糖皮质激素地塞米松产生的效果相似。丝素蛋白纳米粒是白藜芦醇控释的一个有吸引力的策略，显示出免疫调节特性和肠道抗炎作用。
We aimed to evaluate the intestinal anti-inflammatory properties of silk fibroin nanoparticles, around 100 nm in size, when loaded with the stilbene compound resveratrol, in an experimental model of rat colitis. Nanoparticles were loaded with resveratrol by adsorption. The biological effects of the resveratrol-loaded nanoparticles were tested both in vitro, in a cell culture of RAW 264.7 cells (mouse macrophages), and in vivo, in the trinitrobenzenesulfonic acid model of rat colitis, when administered intracolonically. The resveratrol liberation in 1× phosphate-buffered saline (PBS; pH 7.4) was characterized by fast liberation, reaching the solubility limit in 3 hours, which was maintained over a period of 80 hours. The in vitro assays revealed immunomodulatory properties exerted by these resveratrol-loaded nanoparticles since they promoted macrophage activity in basal conditions and inhibited this activity when stimulated with lipopolysaccharide. The in vivo experiments showed that after evaluation of the macroscopic symptoms, inflammatory markers, and intestinal barrier function, the fibroin nanoparticles loaded with resveratrol had a better effect than the single treatments, being similar to that produced by the glucocorticoid dexamethasone. Silk fibroin nanoparticles constitute an attractive strategy for the controlled release of resveratrol, showing immunomodulatory properties and intestinal anti-inflammatory effects.