Biomedical Division, State Key Laboratory of Luminescent Materials and Devices, Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, College of Materials Science and Engineering, South China University of Technology, Guangzhou, 510640, China.
Adv Healthc Mater. 2022 Nov;11(22):e2201544. doi: 10.1002/adhm.202201544. Epub 2022 Sep 18.
Ulcerative colitis (UC) is a prevalent idiopathic inflammatory disease which causes such complications as intestinal perforation, obstruction, and bleeding, and thus deleteriously impacting people's normal work and quality of life. Hence, accurate diagnosis of UC is crucial in terms of planning optimal treatment plan. Herein, a pH/reactive oxygen species (ROS) dual-responsive nanosystem (BM@EP) is developed for UC's detection and therapy. BM@EP is composed of a chromophore-drug dyad and the enteric coating. The chromophore-drug dyad (BOD-XT-DHM) is synthesized by linking the chromophore (BOD-XT-BOH) and a flavonoid drug (dihydromyricetin DHM) through boronate ester bond. The enteric coating includes Eudragit S100 and poly(lactic-co-glycolic acid) (PLGA), the former is commonly employed as a pH-dependent polymer coating excipient so as to attain colon-targeted delivery, and the latter has been widely used as an excipient for the controlled-extended release. After oral administration, BM@EP delivers the dyad (BOD-XT-DHM) into the colon and releases the dyad molecules by being triggered by the alkaline pH in t colon, thereafter upon being stimulated by overexpressed H O in the inflamed colon, the boronate bond in the dyad is broken down and correspondingly the drug DHM is released for UC therapy, simultaneously the chromophore is released for near-infrared second window (NIR-II) fluorescence and optoacoustic imaging for UC diagnosis and recovery evaluation.
溃疡性结肠炎（UC）是一种常见的特发性炎症性疾病，可导致肠道穿孔、梗阻和出血等并发症，从而严重影响人们的正常工作和生活质量。因此，UC 的准确诊断对于制定最佳治疗方案至关重要。在此，开发了一种 pH/活性氧（ROS）双重响应纳米系统（BM@EP）用于 UC 的检测和治疗。BM@EP 由发色团-药物偶联物和肠溶性涂层组成。发色团-药物偶联物（BOD-XT-DHM）通过硼酸酯键将发色团（BOD-XT-BOH）和黄酮类药物（二氢杨梅素 DHM）连接合成。肠溶性涂层包括 Eudragit S100 和聚乳酸-共-羟基乙酸（PLGA），前者通常用作 pH 依赖性聚合物涂层赋形剂，以实现结肠靶向递送，后者已广泛用作控制释放的赋形剂。口服给药后，BM@EP 将偶联物（BOD-XT-DHM）递送到结肠，并在结肠的碱性 pH 下被触发释放偶联物分子，随后在炎症结肠中过表达的 H2O2 的刺激下，偶联物中的硼酸酯键被破坏，相应地释放药物 DHM 用于 UC 治疗，同时释放发色团用于近红外二区（NIR-II）荧光和光声成像以进行 UC 诊断和恢复评估。
