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具有抗胃酸和缓释功能的黏膜黏附性水凝胶,用于改善 DSS 诱导的溃疡性结肠炎。

Mucoadhesive Hydrogel with Anti-gastric Acid and Sustained-Release Functions for Amelioration of DSS-Induced Ulcerative Colitis.

机构信息

School of Food Science and Technology, Dalian Polytechnic University, Dalian 116034, China.

Collaborative Innovation Center of Seafood Deep Processing, Dalian Polytechnic University, Dalian 116034, China.

出版信息

J Agric Food Chem. 2023 Mar 8;71(9):4016-4028. doi: 10.1021/acs.jafc.2c07777. Epub 2023 Feb 22.

Abstract

Mucoadhesive hydrogels with multifunctional properties such as gastric acid resistance and sustained drug release in the intestinal tract are highly desirable for the oral treatment of inflammatory bowel diseases (IBDs). Polyphenols are proven to have great efficacies compared with the first-line drugs for IBD treatments. We recently reported that gallic acid (GA) was capable of forming a hydrogel. However, this hydrogel is prone to easy degradation and poor adhesion . To tackle this problem, the current study introduced sodium alginate (SA) to form a gallic acid/sodium alginate hybrid hydrogel (GAS). As expected, the GAS hydrogel showed excellent antiacid, mucoadhesive, and sustained degradation properties in the intestinal tract. studies demonstrated that the GAS hydrogel significantly alleviated ulcerative colitis (UC) in mice. The colonic length of the GAS group (7.75 ± 0.38 cm) was significantly longer than that of the UC group (6.12 ± 0.25 cm). The disease activity index (DAI) value of the UC group was (5.5 ± 0.57), which was markedly higher than that of the GAS group (2.5 ± 0.65). The GAS hydrogel also could inhibit the expression of inflammatory cytokines, regulating macrophage polarization and improving the intestinal mucosal barrier functions. All these results indicated that the GAS hydrogel was an ideal candidate for oral treatment of UC.

摘要

具有多重功能的黏膜黏附水凝胶,如在胃肠道中具有抗胃酸和持续药物释放的功能,是治疗炎症性肠病(IBD)的口服治疗的理想选择。多酚类化合物被证明比 IBD 治疗的一线药物具有更大的疗效。我们最近报道了没食子酸(GA)能够形成水凝胶。然而,这种水凝胶容易降解且黏附性差。为了解决这个问题,本研究引入海藻酸钠(SA)来形成没食子酸/海藻酸钠杂化水凝胶(GAS)。正如预期的那样,GAS 水凝胶在胃肠道中表现出优异的抗酸、黏膜黏附性和持续降解特性。研究表明,GAS 水凝胶显著缓解了小鼠的溃疡性结肠炎(UC)。GAS 组的结肠长度(7.75 ± 0.38 cm)明显长于 UC 组的结肠长度(6.12 ± 0.25 cm)。UC 组的疾病活动指数(DAI)值为(5.5 ± 0.57),明显高于 GAS 组的(2.5 ± 0.65)。GAS 水凝胶还可以抑制炎症细胞因子的表达,调节巨噬细胞极化,改善肠道黏膜屏障功能。所有这些结果表明,GAS 水凝胶是治疗 UC 的口服治疗的理想候选物。

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