Inflammatory bowel disease (IBD) is a chronic intestinal disease with painful clinical manifestations and high risks of cancerization. With no curative therapy for IBD at present, the development of effective therapeutics is highly advocated. Drug delivery systems have been extensively studied to transmit therapeutics to inflamed colon sites through the enhanced permeability and retention (EPR) effect caused by the inflammation. However, the drug still could not achieve effective concentration value that merely utilized on EPR effect and display better therapeutic efficacy in the inflamed region because of nontargeted drug release. Substantial researches have shown that some specific receptors and cell adhesion molecules highly expresses on the surface of colonic endothelial and/or immune cells when IBD occurs, ligand-modified drug delivery systems targeting such receptors and cell adhesion molecules can specifically deliver drug into inflamed sites and obtain great curative effects. This review introduces the overexpressed receptors and cell adhesion molecules in inflamed colon sites and retrospects the drug delivery systems functionalized by related ligands. Finally, challenges and future directions in this field are presented to advance the development of the receptor-mediated targeted drug delivery systems for the therapy of IBD.

炎症性肠病（IBD）是一种慢性肠道疾病，具有痛苦的临床表现和癌变的高风险。由于目前 IBD 尚无根治性治疗方法，因此大力提倡开发有效的治疗方法。药物递送系统已被广泛研究以通过炎症引起的增强的渗透性和保留 (EPR) 效应将治疗药物传输到发炎的结肠部位。然而，由于药物非靶向释放，该药物仍无法达到仅利用EPR效应的有效浓度值，并在炎症区域显示出更好的治疗效果。大量研究表明，当IBD发生时，某些特异性受体和细胞粘附分子在结肠内皮和/或免疫细胞表面高表达，针对此类受体和细胞粘附分子的配体修饰药物递送系统可以将药物特异性递送至炎症部位并获得很好的疗效。本综述介绍了发炎结肠部位的过度表达受体和细胞粘附分子，并回顾了由相关配体功能化的药物递送系统。最后，提出了该领域的挑战和未来方向，以推进用于 IBD 治疗的受体介导的靶向给药系统的开发。