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Recent advances in mesalamine colonic delivery systems
Future Journal of Pharmaceutical Sciences Pub Date : 2020-07-31 , DOI: 10.1186/s43094-020-00057-7
Mohammad F. Bayan , Rana F. Bayan

Increased attention has been focused on the continuous development and improvement of mesalamine colonic specific delivery systems, for the effective treatment of inflammatory bowel diseases; thus enhancing therapeutic efficacy and reducing potential side effects. Mesalamine is a class IV drug, according to the Biopharmaceutics Classification System, used usually to treat inflammation associated with colon related diseases such as Crohn’s disease and ulcerative colitis. Main text An ideal colon targeting system aims to deliver a therapeutic agent, selectively and effectively, to the colon. This system should ideally retain the drug release in the upper GI tract (stomach and small intestine); while trigger the drug release in the colon. Several approaches have been used to fabricate formulations to achieve a colon specific delivery of mesalamine such as; time dependent, pH responsive, enzymatic/microbial responsive and ultrasound mediated approaches. This overview outlines the recent advances in mesalamine-colon delivery approaches for the potential treatment of ulcerative colitis and Crohn’ disease. A combined pH-time dependent delivery system can improve mesalamine colonic drug delivery via employing carriers capable of retarding mesalamine release in the stomach and delivering it at predetermined time points after entering the intestine. The existence of specific enzymes, produced by various anaerobic bacteria present in the colon advocates the advantage of designing enzyme sensitive systems and combining it with pH-time dependent system to improve mesalamine colonic delivery. The use of ultrasound has shown promises to effectively treat inflammatory bowel diseases.

中文翻译:

美沙拉敏结肠输送系统的最新进展

为了有效治疗炎症性肠病,人们越来越关注美沙拉敏结肠特异性递送系统的不断发展和改进。从而提高治疗效果并减少潜在的副作用。根据生物制药分类系统,美沙拉敏是IV类药物,通常用于治疗与结肠相关疾病(例如克罗恩氏病和溃疡性结肠炎)相关的炎症。理想的结肠靶向系统旨在将治疗剂选择性地和有效地递送至结肠。理想情况下,该系统应将药物释放到上消化道(胃和小肠)中。同时触发药物在结肠中释放。已经使用了几种方法来制备制剂,以实现美沙明胺的结肠特异性递送,例如 时间依赖性,pH响应,酶/微生物响应和超声介导的方法。该概述概述了美沙拉胺-结肠递送方法在溃疡性结肠炎和克罗恩病潜在治疗中的最新进展。结合pH-时间依赖性的递送系统可通过采用能够延缓美沙拉胺在胃中释放并在进入肠道后的预定时间点递送的载体来改善美沙拉敏结肠药物的递送。由结肠中存在的各种厌氧细菌产生的特定酶的存在提倡设计酶敏感系统并将其与pH时间依赖性系统结合以改善美沙拉敏结肠递送的优势。
更新日期:2020-07-31
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