Department of Emergency, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325035, People's Republic of China.
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 325035, People's Republic of China.
Int J Nanomedicine. 2021 Dec 20;16:8235-8250. doi: 10.2147/IJN.S344805. eCollection 2021.
Gastric ulcers (GU) are a disease of the gastrointestinal tract that can be caused by excessive alcohol consumption and heavy use of nonsteroidal anti-inflammatory drugs. GU manifests predominantly as pathological damage, such as extensive inflammatory erosion and superficial bleeding of the gastric mucosa. Oxidative stress damage and the inflammatory response are now considered important predisposing factors for GU, suggesting that antioxidant and anti-inflammatory drugs could be treatments for GU. Nanoparticle drug carriers offer many advantages over conventional drugs, such as improved drug efficiency, increased drug stability, and increased half-life.
We designed chitosan-bilirubin conjugate (CS-BR) nanoparticles and assessed the anti-inflammatory and antioxidant abilities of CS-BR in gastric epithelial cells. Then, we evaluated the intragastric retention time and the anti-ulcer effects of CS-BR in vivo.
The in vitro data showed that CS-BR nanoparticles protect gastric epithelial cells against oxidative/inflammatory injury. The in vivo study demonstrated that CS-BR nanoparticles accumulate permanently in the stomach and exert powerful antioxidant and anti-inflammatory effects against GU.
This study applied bilirubin to the treatment of GU and confirmed that CS-BR nanoparticles are effective at alleviating acute GU in an experimental model. The findings provide innovative ideas for prophylaxis against or treatment of GU.
胃溃疡(GU)是一种胃肠道疾病,可由过量饮酒和大量使用非甾体抗炎药引起。GU 主要表现为病理性损伤,如胃黏膜广泛炎症侵蚀和浅表出血。氧化应激损伤和炎症反应被认为是 GU 的重要诱发因素,这表明抗氧化和抗炎药物可能是 GU 的治疗方法。纳米药物载体比传统药物具有许多优势,例如提高药物效率、增加药物稳定性和延长半衰期。
我们设计了壳聚糖-胆红素缀合物(CS-BR)纳米粒子,并评估了 CS-BR 在胃上皮细胞中的抗炎和抗氧化能力。然后,我们评估了 CS-BR 在体内的胃内滞留时间和抗溃疡作用。
体外数据表明,CS-BR 纳米粒子可保护胃上皮细胞免受氧化/炎症损伤。体内研究表明,CS-BR 纳米粒子在胃中永久积聚,并对 GU 发挥强大的抗氧化和抗炎作用。
本研究将胆红素应用于 GU 的治疗,并证实 CS-BR 纳米粒子可有效缓解实验模型中的急性 GU。研究结果为预防或治疗 GU 提供了创新思路。