Recently, active targeting using nanocarriers with biological ligands has emerged as a novel strategy for improving the delivery of therapeutic and/or imaging agents to tumor cells. The presence of active targeting moieties on the surface of nanomedicines has been shown to play an important role in enhancing their accumulation in tumoral cells and tissues versus healthy ones. This property not only helps to increase the therapeutic index but also to minimize possible side effects of the designed nanocarriers. Since the overexpression of epidermal growth factor receptors (EGFR) is a common occurrence linked to the progression of a broad variety of cancers, the potential application of anti-EGFR immunotherapy and EGFR-targeting ligands in active targeting nanomedicines is getting increasing attention. Henceforth, the EGFR-targeted nanomedicines were extensively studied in vitro and in vivo but exhibited both satisfactory and disappointing results, depending on used protocols. This review is designed to give an overview of a variety of EGFR-targeting ligands available for nanomedicines, how to conjugate them onto the surface of nanoparticles, and the main analytical methods to confirm this successful conjugation.