Currently, many therapies fail due to an insufficient drug dose reaching the target site and high systemic toxicity. Protein-based drug delivery systems that allow an increase in drug concentration at a specific location in the body or predominantly target malignant cells are promising technologies. Due to the high need for iron in many disorders including various types of cancer, iron-binding proteins: transferrin, ferritin and hemoglobin, are a promising tool as drug carriers. In this review we summarize the characteristics of human iron-binding proteins and present their use in targeted drug delivery strategies.