Therapeutic effect of indirubin-loaded bovine serum albumin nanoparticules on ulcerative colitis.
Therapeutic effect of indirubin-loaded bovine serum albumin nanoparticules on ulcerative colitis.
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靛玉红纳米粒对溃疡性结肠炎的治疗作用。
DOI：
10.1039/d1bm01896e
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发表时间：
2022-03
影响因子：
6.6
通讯作者：
Guang-Min Yu;Li-feng Zhou;Xiaoming Liu;Bin Liu;Xue-Ying Lai;Chunxia Xu;Ming-Yi Long;Yan-Ming Zhu;Jide Wang;Ming-Song Li
中科院分区：
文献类型：
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作者：
Guang-Min Yu;Li-feng Zhou;Xiaoming Liu;Bin Liu;Xue-Ying Lai;Chunxia Xu;Ming-Yi Long;Yan-Ming Zhu;Jide Wang;Ming-Song Li
蓝宝石被认为在治疗溃疡性结肠炎(UC)方面有很大的潜力。但其水溶性差，生物利用度低，限制了其临床应用。制备了载药牛血清白蛋白纳米粒(INPs)，并对其药物包封率、载药量、体外释药能力和短期物理稳定性进行了研究。我们还研究了INPS在小鼠体内的药代动力学。然后，我们比较了INPS和Indiruin对葡聚糖硫酸钠诱导的小鼠结肠炎的疗效，以及来自UC患者的3D培养活检组织。在小鼠模型中，INP治疗的结果，包括疾病活动性指数和血清IL-1β和IL-10水平，明显不同于靛玉红治疗。同样，当我们在UC患者的体外结肠组织中应用INPS和Indiruin时，对于大多数抗氧化和抗炎生物标志物，INPS的作用比Indiruin更强。动物实验和体外实验结果均表明，载体系统进一步增强了靛玉红的治疗效果，使其成为治疗UC的极具前景的候选药物。
Indirubin is considered to have promising potential in the treatment of ulcerative colitis (UC). However, poor aqueous solubility and low bioavailability limit its clinical application. We produced indirubin-loaded bovine serum albumin nanoparticles (INPs) and characterized their drug encapsulation efficiency, drug-loading capacity, capacity to release indirubin in vitro and short-term physical stability. We also investigated the pharmacokinetics of INPs in mice. We then compared the curative effects of INPs and indirubin against dextran sulfate sodium-induced colitis in mice and 3D cultured biopsies from patients with UC. In the mouse model, the outcomes of INP treatment, including the disease activity index and serous levels of interleukin (IL)-1β and IL-10, were significantly different from those of indirubin treatment. Similarly, when we administered INPs and indirubin to the ex vivo colonic tissues of patients with UC, the effect of INPs was stronger than that of indirubin for most antioxidant and anti-inflammatory biomarkers. The results of both the animal trial and ex vivo experiment indicate that the therapeutic effect of indirubin was further enhanced by the carrier system, making it a highly promising medical candidate for UC.