Centre for Research in Medical Devices (CÚRAM), National University of Ireland Galway, Newcastle, Galway, Ireland.
Centre for Research in Medical Devices (CÚRAM), National University of Ireland Galway, Newcastle, Galway, Ireland.
Adv Drug Deliv Rev. 2019 Jun;146:248-266. doi: 10.1016/j.addr.2018.06.021. Epub 2018 Jul 5.
Oral colon-specific delivery systems emerged as the main therapeutic cargos by making a significant impact in the field of modern medicine for local drug delivery in intestinal inflammation. The site-specific delivery of therapeutics (aminosalicylates, glucocorticoids, biologics) to the ulcerative mucus tissue can provide prominent advantages in mucosal healing (MH). Attaining gut mucosal healing and anti-fibrosis are main treatment outcomes in inflammatory bowel disease (IBD). The pharmaceutical strategies that are commonly used to achieve a colon-specific drug delivery system include time, pH-dependent polymer coating, prodrug, colonic microbiota-activated delivery systems and a combination of these approaches. Amongst the different approaches reported, the use of biodegradable polysaccharide coated systems holds great promise in delivering drugs to the ulcerative regions. The present review focuses on major physiological gastro-intestinal tract challenges involved in altering the pharmacokinetics of delivery systems, pathophysiology of MH and fibrosis, reported drug-polysaccharide cargos and focusing on conventional to advanced disease responsive delivery strategies, highlighting their limitations and future perspectives in intestinal inflammation therapy.
口服结肠特异性递药系统通过在局部肠道炎症的现代医学领域中对局部药物递送产生重大影响，成为主要的治疗载体。将治疗药物（氨基水杨酸盐、糖皮质激素、生物制剂）递送到溃疡性黏液组织的部位特异性给药，可以在黏膜愈合（MH）方面提供显著优势。在炎症性肠病（IBD）中，实现肠道黏膜愈合和抗纤维化是主要的治疗终点。用于实现结肠特异性药物递送系统的常见药物策略包括时间、pH 依赖性聚合物涂层、前药、结肠微生物群激活的递送系统以及这些方法的组合。在报道的不同方法中，使用可生物降解的多糖涂层系统在将药物递送到溃疡性区域方面具有很大的潜力。本综述重点介绍了改变递药系统药代动力学、MH 和纤维化的生理学胃肠道挑战、报告的药物-多糖载体，并重点介绍了常规到先进疾病反应性递药策略，突出了它们在肠道炎症治疗中的局限性和未来前景。
