Nanoparticles are increasingly becoming indispensable tool of modern day research in almost every field of science. Cancer nanotechnology has become a prime field of investigations for the scientists nowadays. There are several nanocarrier systems used for effective cancer therapeutic and gold nanoparticles have become promising vehicles for the delivery of anticancer drugs into their targets. Gold nanospheres, nanorods, nanoshells, nanocages, and surface enhanced Raman scattering nanoparticles will be discussed in detail regarding their uses in in vitro assays, ex vivo and in vivo imaging, cancer therapy, and drug delivery. Gold nanoparticles are widely used in many fields as preferred materials for their unique optical and physical properties such as surface plasmon oscillations for labelling, imaging and sensing.Much advancement was made in biomedical applications with better biocompatibility in disease diagnosis and therapeutics. Multifunctionality is the key feature of nanoparticle-based agents.