Nanotherapeutics has the potential of providing limitless opportunities in the area of drug and gene delivery for treatment of cancer. Although the path toward commercialization of nanoparticulate oncology drugs is long and carries significant risks, there is still considerable excitement for utilizing nanoparticle technologies in cancer drug development. Recently, there has been a significant growth in the number of nanoparticle delivery systems, used in clinical trials. Several incorporations have been established between pharmaceutical and nanotechnology companies striving to understand, develop and utilize effective interactions between nanomaterials and biological systems for cancer treatment by means of colloidal delivery systems. Protein-based nanoparticles, with one already approved and several under-development products in the commercial market, are of the pioneers of the successful employment of nanoparticulate systems in improving the cancer treatment techniques. The main reason behind the widely tendency to the usage of protein-based systems is their possibility of functionalization, biocompatibility, nonimmunogenicity, and high loading capacity for both hydrophobic and hydrophilic therapeutics. The aim of this review is to provide a comprehensive overview on the most recent findings in the area of utilization of protein-based nanoparticles for delivery of anticancer agents, as well as interpretation of the challenges encountered in the field.