Abstract

The effective delivery of therapeutic agents to their target sites within the human body is a complex endeavor that relies on a myriad of intricate processes. Central to this challenge are the cellular gateways, specialized membrane transport proteins that regulate the movement of molecules across cell membranes. These gatekeepers, known as drug transporters, play a pivotal role in modulating the absorption, distribution, and excretion of drugs and other molecules. As such, understanding the functioning and regulation of drug transporters is paramount for optimizing therapeutic delivery strategies and enhancing drug efficacy. As the field continues to evolve, researchers are uncovering novel strategies to exploit drug transporters for targeted drug delivery and enhanced therapeutic outcomes. We discuss current approaches that leverage transporter-mediated drug delivery systems, including prodrugs, nanoparticles, and carrier-mediated transport.