Ligand-mediated active targeting for enhanced oral absorption

• Published in: Drug discovery today Vol. 19; no. 7; pp. 898 - 904
• Main Authors: Zhang, Xingwang, Wu, Wei
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-07-2014
• Subjects: Administration, Oral; Animals; Biological Availability; Drug Delivery Systems - methods; Humans; Intestinal Absorption - drug effects; Intestinal Absorption - physiology; Intestinal Mucosa - drug effects; Intestinal Mucosa - metabolism; Ligands; Pharmaceutical Preparations - administration & dosage; Pharmaceutical Preparations - metabolism
• ISSN: 1359-6446; 1878-5832
• DOI: 10.1016/j.drudis.2014.03.001

•Targeting the intestinal epithelia is a new strategy to enhance oral absorption of drugs.•Breakthroughs in this field will advance the development in oral drug delivery.•The transenterocytic pathway should be explored.•New insights into gut biology will enlighten development in this field.
Although the oral route is the most popular and acceptable way of drug administration owing to good patient compliance and safety, oral drug delivery is faced with continuous challenges regarding poorly soluble, poorly permeable or gastrointestinally unstable drugs such as proteins and polypeptides. The overall bioavailability and therapeutic effect still needs to be further improved by innovative delivery technologies. Recently, various novel strategies, for instance using ligand-decorated carriers, have been investigated for delivery of poorly absorptive therapeutics orally. In this review, we will discuss the state of the art of ligand-mediated targeting to intestinal epithelia for oral delivery of drugs with low bioavailability.