BACKGROUND: Carcinoma of the prostate gland (PCa) is one of the most commonly diagnosed cancer diseases among men around the world. PCa has become the major considerable health and epidemic problem which causes death in men with a high prevalence and relatively lower mortality risk. The inability of conventional diagnosis tools to detect cancer at an early and potentially curable stage further hinders effective treatment options and spur demand for improved technologies. Nanoparticles are emerging as a versatile tool for disease diagnosis to therapy. Gold nanoparticles (AuNPs) have a huge potential in targeted drug delivery and detection of cancerous cells. Diverse predominant distinctive properties of gold nanomaterials and their effective functionalization make them a suitable material for early diagnosis and effective treatment of cancer. OBJECTIVE: To summarize the recent research and patents on the development of multifunctional AuNPs based nanoformulations for early diagnosis and targeted drug delivery to prostate cancer. Further, discussion on the salient features of gold nanostructures and its evaluation of extremely attractive vectors in prostate cancer diagnosis and treatments. CONCLUSION: This review summarizes the use of AuNPs based nanoformulations in cancer diagnostics and therapy, which has been recognized as an important platform as smart materials for clinical application. The ability to tune the size, shape and the physical properties of AuNPs along with their low toxicity, biocompatibility and large surface chemistry makes them as a promising candidate for clinical use.