Lozano-Pérez Antonio Abel, Rodriguez-Nogales Alba, Ortiz-Cullera Víctor, Algieri Francesca, Garrido-Mesa José, Zorrilla Pedro, Rodriguez-Cabezas M Elena, Garrido-Mesa Natividad, Utrilla M Pilar, De Matteis Laura, de la Fuente Jesús Martínez, Cenis José Luis, Gálvez Julio
Instituto Murciano de Investigación y Desarrollo Agrario y Alimentario, Murcia, Spain.
Centro de Investigaciones Biomédicas en Red - Enfermedades Hepáticas y Digestivas, Department of Pharmacology, ibs Granada, Center for Biomedical Research, University of Granada, Granada, Spain.
Int J Nanomedicine. 2014 Sep 23;9:4507-20. doi: 10.2147/IJN.S68526. eCollection 2014.
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.
我们旨在评估在大鼠结肠炎实验模型中,负载二苯乙烯化合物白藜芦醇的、尺寸约为100纳米的丝素蛋白纳米颗粒的肠道抗炎特性。
通过吸附法将白藜芦醇负载到纳米颗粒上。将负载白藜芦醇的纳米颗粒的生物学效应在体外(在RAW 264.7细胞(小鼠巨噬细胞)的细胞培养中)和体内(在大鼠结肠炎的三硝基苯磺酸模型中,通过结肠内给药)进行测试。
负载白藜芦醇的纳米颗粒在1×磷酸盐缓冲盐水(PBS;pH 7.4)中的释放特点是快速释放,在3小时内达到溶解度极限,并在80小时内保持这一水平。体外试验显示,这些负载白藜芦醇的纳米颗粒具有免疫调节特性,因为它们在基础条件下促进巨噬细胞活性,而在用脂多糖刺激时则抑制这种活性。体内实验表明,在评估宏观症状、炎症标志物和肠道屏障功能后,负载白藜芦醇的丝素蛋白纳米颗粒比单一治疗效果更好,与糖皮质激素地塞米松产生的效果相似。
丝素蛋白纳米颗粒是白藜芦醇控释的一种有吸引力的策略,具有免疫调节特性和肠道抗炎作用。