炎症性肠病(IBD)是一种慢性肠道疾病,临床表现痛苦,癌变风险高。目前没有治疗IBD的治疗方法,大力提倡开发有效的疗法。已经广泛研究了药物递送系统,以通过由炎症引起的增强的渗透性和保留(EPR)效应将治疗剂传递到发炎的结肠部位。然而,由于非靶向药物释放,该药物仍然无法达到仅利用EPR效应的有效浓度值,并且在发炎区域显示出更好的治疗效果.大量研究表明,IBD发生时,一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,靶向此类受体和细胞粘附分子的配体修饰的药物递送系统可以特异性地将药物递送到发炎部位并获得巨大的疗效。本文介绍了结肠炎症部位过表达的受体和细胞粘附分子,并回顾了相关配体功能化的药物传递系统。最后,提出了该领域的挑战和未来方向,以推进用于治疗IBD的受体介导的靶向药物递送系统的开发。
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.