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用于靶向炎症性肠黏膜的纳米和微粒药物载体。

Nano- and microparticulate drug carriers for targeting of the inflamed intestinal mucosa.

机构信息

Helmholtz-Institute for Pharmaceutical Research Saarland, Dept. of Drug Delivery Saarland University, Campus A 4 1, 66123 Saarbrücken, Germany.

出版信息

J Control Release. 2012 Jul 20;161(2):235-46. doi: 10.1016/j.jconrel.2012.01.028. Epub 2012 Jan 25.

Abstract

Conventional treatment of inflammatory bowel disease (IBD) is based on the daily administration of high doses of immune-suppressant or anti-inflammatory drugs, often complicated by serious adverse effects. Thus, a carrier system that delivers the drug specifically to the inflamed intestinal regions and shows prolonged drug release would be desirable. The advent of TNF-α antibodies and other biopharmaceuticals as potent and specific immune modulators in recent years has broadened the treatment options in IBD, but further increases the necessity for adequate drug delivery, as integrity and bioactivity of the biological active have to be ensured. Exploiting the pathophysiological idiosyncrasies of IBD such as increased mucus production, changes in the structure of the intestinal epithelium and invasion of activated macrophages, different colloidal drug carrier systems have been designed to passively or actively target the site of inflammation. This review introduces different micro- or nanoparticulate drug delivery systems for oral application in IBD therapy for the delivery of small molecular compounds and next generation therapeutics from the group of biological (i.e. peptide and nucleotide based) drugs.

摘要

炎症性肠病(IBD)的常规治疗方法基于每日大剂量使用免疫抑制剂或抗炎药物,这常常导致严重的不良反应。因此,人们希望有一种载药系统能够将药物特异性递送到炎症肠道区域,并具有延长的药物释放。近年来,TNF-α 抗体和其他生物制药作为有效的、特异性的免疫调节剂的出现,拓宽了 IBD 的治疗选择,但进一步增加了对充分药物输送的需求,因为必须确保生物活性的完整性和生物活性。利用 IBD 的病理生理特征,如增加黏液分泌、肠上皮结构改变和活化巨噬细胞浸润,设计了不同的胶体药物载体系统,以被动或主动靶向炎症部位。本文介绍了不同的微纳米药物传递系统,用于治疗 IBD 的口服应用,以递送小分子化合物和新一代生物治疗药物(如肽类和核苷酸类药物)。

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