Haupt Susan, Rubinstein Abraham
The Hebrew University of Jerusalem, Faculty of Medicine, School of Pharmacy, Jerusalem, Israel.
Crit Rev Ther Drug Carrier Syst. 2002;19(6):499-551. doi: 10.1615/critrevtherdrugcarriersyst.v19.i6.10.
Oral administration offers a potential portal to the superficial layers of the gastrointestinal (GI) tract (local delivery) and to the blood and lymphatics (systemic delivery). The harsh hydrolytic environment of the GI tract and the epithelial barriers to absorption, however, pose major challenges to the success of this mode of drug delivery for peptide and protein drugs. One approach to minimizing enzymatic degradation in the GI tract is to target drugs to the apparently less proteolytically active colon. In this review, the evidence supporting the colon as an attractive site for peptide and protein drug delivery will be discussed. The discussion will be confined to specific examples of delivery systems bearing both peptides and proteins that have been tested in the colonic context.
口服给药为胃肠道表层（局部给药）以及血液和淋巴管（全身给药）提供了一个潜在途径。然而，胃肠道恶劣的水解环境以及上皮吸收屏障，对肽类和蛋白质类药物这种给药方式的成功构成了重大挑战。减少胃肠道中酶降解的一种方法是将药物靶向到蛋白水解活性明显较低的结肠。在这篇综述中，将讨论支持结肠作为肽类和蛋白质类药物给药的理想部位的证据。讨论将局限于在结肠环境中已测试过的同时含有肽类和蛋白质类的给药系统的具体实例。
