Current approaches to drug delivery rely heavily on the increased metabolism of diseased cells to uptake circulating therapeutics at a higher rate than healthy cells. However, unwanted drug delivery to healthy cells occurs, resulting in undesired side effects. These deleterious side effects limit the use, dosage, and therapeutic course of drugs, limiting their full potential. In addition, side effects resulting from drug delivery to healthy cells and tissue are a major cause for dismissal from clinical trials, limiting the number of new FDA approved drugs. Methods to deliver small molecule, macromolecule, and nanoparticle-based therapeutics selectively to diseased cells and tissue are extremely valuable. Such reagents would decrease unwanted cytotoxic side effects associated with untargeted drug delivery, and would permit lower dosage levels, resulting in a reduction in therapeutic costs.

In addition to targeted therapeutic delivery, methods for selectively delivering bio-imaging dyes and agents to diseased cells would increase the imaging contrast ratio between diseased and healthy tissue, simplifying diagnosis and surgical efforts.

Researchers in The McNaughton Group use selection-based approaches to identify materials capable of selectively targeting the delivery of therapeutics and imaging reagents to diseased cells. After evolving cell-selective delivery reagents, the utility of these reagents is examined ex vivo and in vivo (Fig 1).