Oral colon delivery of insulin with the aid of functional adjuvants

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• 作者：Alessandra Maroni ; Lucia Zema ; Maria Dorly Del Curto ; Anastasia Foppoli ; Andrea Gazzaniga ; ^{andrea.gazzaniga@unimi.it}
• 关键词：IBD ; inflammatory bowel disease ; GI ; gastrointestinal ; GALT ; gut-associated lymphoid tissue ; CFU ; colony-forming unit ; SITT ; small intestinal transit time ; SE ; standard error ; HPMC ; hydroxypropylmethylcellulose ; HEC ; hydroxyethylcellulose ; HPC ; hydroxypro
• 刊名：Advanced Drug Delivery Reviews
• 出版年：2012
• 期刊代码：2_0169409x
• 类别：bio
• 出版时间：1 May, 2012
• 卷：64
• 期：6
• 页码：540-556
• 文件大小：346 K

摘要

Oral colon delivery is currently considered of importance not only for the treatment of local pathologies, such as primarily inflammatory bowel disease (IBD), but also as a means of accomplishing systemic therapeutic goals. Although the large bowel fails to be ideally suited for absorption processes, it may indeed offer a number of advantages over the small intestine, including a long transit time, lower levels of peptidases and higher responsiveness to permeation enhancers. Accordingly, it has been under extensive investigation as a possible strategy to improve the oral bioavailability of peptide and protein drugs. Because of a strong underlying rationale, most of these studies have focused on insulin. In the present review, the impact of key anatomical and physiological characteristics of the colon on its viability as a protein release site is discussed. Moreover, the main formulation approaches to oral colon targeting are outlined along with the design features and performance of insulin-based devices.