Intestinal membrane transporter-mediated approaches to improve oral drug delivery

Abstract

Effective oral delivery of drugs remains a major challenge given their possible undesirable physicochemical properties, physicochemical factors, and the physiological conditions of the gastrointestinal (GI) tract. Continuous efforts have been made to overcome these issues by improving the intestinal permeability and oral bioavailability of drugs. Recently, the strategy to improve intestinal permeability has shifted towards targeting drugs to intestinal membrane transporters. In this review, the usefulness of various solute carrier (SLC) and ATP (adenosine triphosphate)-binding cassette (ABC) transporters that are widely expressed in the intestinal epithelia and their impact on increasing the membrane permeability and oral bioavailability of drugs are discussed. Targeting intestinal membrane transporters has emerged as a promising avenue to increase the oral absorption of drugs. Recently, several approaches that target intestinal membrane transporters have resulted in significant improvements in oral bioavailability, such as the use of absorption enhancers or excipients, modification of a drug’s physicochemical properties, and/or the development of novel drug delivery vehicles that enhance drug influx and inhibit efflux. Additionally, efforts have been made to elucidate the role of dual-transporter targeting in drug delivery. Therefore, implementation of transporter-mediated drug-delivery strategies may be a promising approach to increase oral bioavailability.