Conventional cancer management is directly associated with many problems, including accurate therapeutic delivery to tumours and serious side effects of chemotherapeutics. A specific and efficient anticancer delivery to the tumour site without damaging normal tissues is the ultimate goal of all cancer treatment strategies. Nano medicine has immense potential for cancer therapy that focuses on improving treatment efficacy, while reducing toxicity to normal tissues as well. However, the bio distribution and targeting capability of nanoparticles lacking targeting ligands rely solely on their physicochemical properties and the pathophysiological parameters of the body. Targeting is a promising strategy for selective and efficient therapeutic delivery to tumour cells with reduced detrimental side effects. Taking advantage of the fact that molecular markers and receptors over-express on the tumour cell surface as compared to a normal cell, the active targeting approach would be beneficial for cancer therapy. The epidermal growth factor receptors (EGFR), abnormally overexpressed in many epithelial tumours, have received much attention for molecular targeting in cancer diagnostics and therapeutics. This review presents the role of EGFR targeting in cancer imaging and therapy, and some recent researches on treatment of EGFR overexpressing cancers by using targeted nano particulate platforms. It also discusses illustrative examples of various ligands, including antibodies, antibody fragments, nano bodies, and peptides.