Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Department of Food Science and Technology, Ferdowsi University of Mashhad, Mashhad, Iran.
Int J Pharm. 2019 Mar 10;558:367-379. doi: 10.1016/j.ijpharm.2019.01.022. Epub 2019 Jan 18.
Site-specific colon drug delivery is a practical approach for the treatment of local diseases of the colon with several advantages such as rapid onset of action and reduction of the dosage of the drug as well as minimization of harmful side effects. 5-aminosalicylic acid (5-ASA) is a drug of choice in the treatment of inflammatory bowel disease and colitis. For the efficient delivery of this drug, it is vital to prevent 5-ASA release in the upper part of the gastrointestinal tract and to promote its release in the proximal colon. Different approaches including chemical manipulation of drug molecule for production of prodrugs or modification of drug delivery systems using pH-dependent, time-dependent and/or bacterially biodegradable materials have been tried to optimize 5-ASA delivery to the colon. In the current review, the different strategies utilized in the design and development of an oral colonic delivery dosage form of 5-ASA are presented and discussed.
靶向结肠递药是一种治疗结肠局部疾病的实用方法,具有起效快、减少药物剂量以及最小化有害副作用等优点。5-氨基水杨酸(5-ASA)是治疗炎症性肠病和结肠炎的首选药物。为了实现这种药物的有效传递,至关重要的是要防止 5-ASA 在胃肠道的上部释放,并促进其在近端结肠中的释放。人们尝试了不同的方法,包括对药物分子进行化学修饰以生产前药,或者使用 pH 依赖性、时间依赖性和/或细菌可生物降解的材料来修饰药物传递系统,以优化 5-ASA 递送到结肠。在本综述中,介绍并讨论了设计和开发 5-ASA 口服结肠递药剂型中使用的不同策略。