Rutin-Loaded Stimuli-Responsive Hydrogel for Anti-Inflammation.
Rutin-Loaded Stimuli-Responsive Hydrogel for Anti-Inflammation.
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DOI：
10.1021/acsami.2c02295
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发表时间：
2022-06
影响因子：
9.5
通讯作者：
Hongyue Wang;Lin Wang;Shasha Guo;Zehao Liu;Luqing Zhao;R. Qiao;C. Li
中科院分区：
文献类型：
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作者：
Hongyue Wang;Lin Wang;Shasha Guo;Zehao Liu;Luqing Zhao;R. Qiao;C. Li
通过刺激响应硼酸酯键将活性类黄酮化合物芦丁掺入鸟苷苯硼酸酯水凝胶（GBR）中，用于治疗炎症性肠病（IBD）。通过核磁共振、紫外可见光谱和原子力显微镜对药物递送系统的成分和形貌进行了表征。流变学测量揭示了所需的可注射性和自愈能力，这有助于其在直肠给药中的应用。细胞分析证明了该系统具有出色的兼容性和安全性，以及形成多细胞聚集体的可能途径。体外药物释放研究表明，该水凝胶在生理介质中表现出良好的稳定性，在酸性pH和含过量ROS的介质中几乎完全释放药物（孵育24 h后药物释放量超过90 wt%），实现了pH/ROS的双响应释放。在结肠炎小鼠模型中，GBR水凝胶的体内活性显示出比游离芦丁更高的治疗效果，并且它可以显着抑制过度表达的炎症细胞因子，包括TNF-α和IL-6。水凝胶的降解研究为其体内应用的安全性提供了进一步的证据。该工作提供了一种简单的策略来制备G-四联体药物载体，有望实现多药物递送。
An active flavonoid compound rutin was incorporated into a guanosine phenylborate hydrogel (GBR) by a stimuli-responsive borate ester linkage for the treatment of inflammatory bowel disease (IBD). The components and morphology of the drug delivery system were characterized by NMR, UV-vis spectroscopy, and AFM. Rheological measurements revealed the required injectability and self-healing ability, which contributed to its application in rectal administration. The cell assays proved the excellent compatibility and safety of the system, and a possible pathway to form multicellular aggregates. In vitro drug-release studies showed that the hydrogel exhibited good stability in physiological medium, and the drug was almost completely released (more than 90 wt % after 24 h of incubation) in acidic pH and excessive ROS-containing medium, realizing the dual-responsive release of pH/ROS. In vivo activities of the GBR hydrogel showed higher therapeutic efficacy than free rutin in a colitis mice model, and it could significantly inhibit overexpressed inflammatory cytokines, including TNF-α and IL-6. Degradation studies of the hydrogel provided further evidence for the safety of its in vivo application. The work provided a simple strategy to prepare a G-quadruplex drug carrier, which was expected to achieve multi-drug delivery.