Cancer is a major cause of mortality and possesses a significant public health threat in the 21st century. Chemotherapy is the most popular method for management of cancer. Nanotechnology offers magnificent benefits for overcoming the drawbacks associated with conventional chemotherapy through the proper entrapment of many potential anti-neoplastic drugs to ensure better tumor targeting. Heparin was used as a carrier in gold and silver nanoparticles which exhibited important biological activities. The heparin coating increases the hydrophilic property of the magnetic nanoparticles that help to attach the cells to the surface of the nanoparticles. Several scientific reports demonstrated that heparin had a significant effect on animal models at metastasis. Heparin/heparin derivative chains are one of the most important tools for formulation of nanoparticles. Compared to other polysaccharides, heparin possesses outstanding pharmacological features like anti-angiogenesis and anti-metastasis which justifies its potential for anticancer therapy.