Department of Gastroenterology, The First Affiliated Hospital of Nanchang University, Nanchang 330006, China.
State Key Laboratory of Silkworm Genome Biology, College of Sericulture, Textile, and Biomass Sciences, Southwest University, Chongqing 400715, China.
Biomolecules. 2022 Sep 8;12(9):1263. doi: 10.3390/biom12091263.
Oral nanoparticles have been considered a prospective drug delivery carrier against ulcerative colitis (UC). To enhance the mucus-penetrating capacity and aqueous solubility, and strengthen the anti-inflammatory effect of resveratrol (RSV), we fabricated RSV-loaded silk fibroin-based nanoparticles with the functionalization of Pluronic F127 (PF-127). The obtained PF-127-functionalized RSV-loaded NPs had an average particle size around 170 nm, a narrow size distribution (polydispersity index < 0.2), and negative zeta potential (−20.5 mV). Our results indicated that the introduction of PF-127 strengthened the mucus-penetrating property of NPs. In vitro studies suggested that NPs with PF-127 enhanced the suppression of the secretion of proinflammatory cytokine TNF-α and reactive oxygen species (ROS) from RAW 264.7 macrophages under lipopolysaccharide stimulation in comparison with other counterparts. According to the evaluation of macro symptoms and main inflammatory cytokines, we further report preferable therapeutic outcomes achieved by PF-127 functionalized-NP-treated dextran sulphate sodium (DSS) groups in the colitis model compared with blank silk fibroin NPs and RSV-loaded NPs without the functionalization of PF-127. Taken together, this work suggests that the fabricated PF-127 NPs via the oral route are promising and useful RSV-loaded nanocarriers for UC treatment.
口服纳米颗粒被认为是一种有前途的药物输送载体，可用于治疗溃疡性结肠炎（UC）。为了增强纳米颗粒的穿透黏液能力和水溶解度，并增强白藜芦醇（RSV）的抗炎效果，我们用具有 PF-127 功能化的丝素蛋白制备了负载 RSV 的纳米颗粒。所得的 PF-127 功能化 RSV 负载 NPs 的平均粒径约为 170nm，粒径分布较窄（多分散指数 < 0.2），且具有负的 zeta 电位（-20.5mV）。我们的结果表明，PF-127 的引入增强了 NPs 的穿透黏液性能。体外研究表明，与其他对照物相比，PF-127 增强了 NPs 对脂多糖刺激下 RAW264.7 巨噬细胞分泌促炎细胞因子 TNF-α和活性氧（ROS）的抑制作用。根据宏观症状和主要炎症细胞因子的评估，我们进一步报告了在结肠炎模型中，与空白丝素蛋白 NPs 和未用 PF-127 功能化的 RSV 负载 NPs 相比，PF-127 功能化-NP 处理的葡聚糖硫酸钠（DSS）组取得了更好的治疗效果。综上所述，该工作表明，通过口服途径制备的 PF-127 NPs 是一种有前途的、用于 UC 治疗的负载 RSV 的纳米载体。
