School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.
Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, Xi'an 710032, China.
J Biomed Nanotechnol. 2022 Jan 1;18(1):120-131. doi: 10.1166/jbn.2022.3233.
As one of the most challenging inflammatory diseases, the incidence of ulcerative colitis (UC) is increasing year by year, but the existing therapeutic drugs are not effective and lack of targeting. Nanomaterials are expected to become promising delivery system due to their good targeting effects. Here, we designed a nanomaterial sensitive to reactive oxygen species, which can be used to treat IBD, especially UC. It is a self-assembled polyether micelle that can be oxidized at the inflammation site where the concentration of reactive oxygen increases, and effectively release the encapsulated budesonide (Bud). Experiments have proved that for DSS-induced colitis, the synthetic drug-loaded nanoparticles have excellent therapeutic effects, can effectively repair intestinal barrier, and significantly improve the damaged colon tissue. At the same time, it has a beneficial regulatory effect on inflammatory factors. Molecular mechanism studies have shown that it achieves its therapeutic effects by activating the peroxisome proliferators-activated receptors- (PPAR-) pathway and inhibiting the nuclear factor (NF)-B pathway. This study proves that oral nano-micelles have an important impact on improving the efficacy of UC treatment drugs and have far-reaching significance for the targeted treatment of gastrointestinal diseases.
作为最具挑战性的炎症性疾病之一，溃疡性结肠炎（UC）的发病率逐年上升，但现有的治疗药物效果不佳且缺乏靶向性。由于具有良好的靶向作用，纳米材料有望成为有前途的药物传递系统。在这里，我们设计了一种对活性氧敏感的纳米材料，可用于治疗 IBD，特别是 UC。这是一种自组装的聚醚胶束，可在活性氧浓度增加的炎症部位被氧化，并有效释放包封的布地奈德（Bud）。实验证明，对于 DSS 诱导的结肠炎，合成载药纳米颗粒具有优异的治疗效果，能有效修复肠道屏障，显著改善受损的结肠组织。同时，对炎症因子具有有益的调节作用。分子机制研究表明，它通过激活过氧化物酶体增殖物激活受体-（PPAR-）途径和抑制核因子（NF）-B 途径来实现其治疗效果。这项研究证明了口服纳米胶束对提高 UC 治疗药物疗效具有重要意义，对胃肠道疾病的靶向治疗具有深远意义。
