Advances in Receptor‐Mediated, Tumor‐Targeted Drug Delivery

Receptor‐mediated drug delivery presents an opportunity to enhance therapeutic efficiency by accumulating drug within the tissue of interest and reducing undesired, off‐target effects. In cancer, receptor overexpression is a platform for binding and inhibiting pathways that shape biodistribution, toxicity, cell binding and uptake, and therapeutic function. This review will identify tumor‐targeted drug delivery vehicles and receptors that show promise for clinical translation based on quantitative in vitro and in vivo data. The authors describe the rationale to engineer a targeted drug delivery vehicle based on the ligand, chemical conjugation method, and type of drug delivery vehicle. Recent advances in multivalent targeting and ligand organization on tumor accumulation are discussed. Revolutionizing receptor‐mediated drug delivery may be leveraged in the therapeutic delivery of chemotherapy, gene editing tools, and epigenetic drugs. The overexpression of receptors on cancerous cells can be exploited for tumor‐targeted drug delivery. The authors discuss the most promising receptor targets and drug delivery vehicles to enhance the therapeutic efficiency by accumulating drugs within a specific tissue. Further, to improve upon current strategies, the rationale for design choices, and ligand surface patterning and density optimization are discussed. .