Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou, 310014, People's Republic of China.
Zhejiang Suichang Limin Pharmaceutical Co. Ltd., Suichang, People's Republic of China.
Pharm Res. 2021 Apr;38(4):693-706. doi: 10.1007/s11095-021-02993-2. Epub 2021 Mar 22.
This study aims to overcome the challenges of the current oral targeted drug delivery system, such as the complex preparation process, poor biocompatibility, and delayed drug release.
Here, a non-covalent polymer hydrogel was prepared using the mechanochemical method, and the solid phase loading of 5-amino salicylic acid (5-ASA) was realized.
The results obtained from the thermodynamics study, particle size analysis, and electron microscopy show that chitosan (CS) and sodium alginate (SA) form a pH-sensitive hydrogel under the mechanochemical force and also maintain good stability in aqueous solution. Fluorescent tracers study showed that the pH-sensitive hydrogel could achieve the targeted drug release in the colon and the retention time was over 12 h. Next, in vivo efficacy studies, change in mice body weight, DAI (disease activity index) score, thymus, and spleen index, and the diseased state of the mice colon revealed that the pH-sensitive hydrogel is an improved drug delivery system over 5-ASA API commercial preparations as observed in the efficacy and toxicological studies.
This method uses an innovative preparation technology that without the need of cross-linking agent to produce an efficient colon-targeted drug delivery system for the treatment of ulcerative colitis.
本研究旨在克服当前口服靶向药物传递系统的挑战，如复杂的制备工艺、较差的生物相容性和延迟的药物释放。
采用机械化学法制备非共价聚合物水凝胶，并实现 5-氨基水杨酸（5-ASA）的固相负载。
热力学研究、粒径分析和电子显微镜的结果表明，壳聚糖（CS）和海藻酸钠（SA）在机械力作用下形成 pH 敏感水凝胶，并且在水溶液中也保持良好的稳定性。荧光示踪研究表明，pH 敏感水凝胶可以在结肠中实现靶向药物释放，保留时间超过 12 小时。接下来，在体内疗效研究中，小鼠体重变化、疾病活动指数（DAI）评分、胸腺和脾脏指数以及小鼠结肠的患病状态表明，与 5-ASA API 商业制剂相比，pH 敏感水凝胶是一种改良的药物传递系统，在疗效和毒理学研究中得到了观察。
该方法使用了一种创新的制备技术，无需使用交联剂即可生产出用于治疗溃疡性结肠炎的高效结肠靶向药物传递系统。
