Due to chemical stability, low toxicity, and relative simplicity of synthesis/modification techniques, gold nanoparticles (NP) enjoy a wide range of biomedical applications, including in vitro diagnostics, targeted drug delivery, contrast-enhanced radiation therapy, and photothermal therapy. The high ratio of the gold NP surface area to their volume facilitates design of complex nanoplatforms for various therapeutic and diagnostic purposes. Unique electrical and optical properties of gold NP known as surface plasmon resonance assist medical diagnosis. In this work we look at the basic methods for gold NP synthesis and modification, including the so-called green chemistry, talk about the pharmacological aspects of their application and highlight their potential as diagnostic agents. We believe that due to their unique properties, gold-based nanoplatforms for targeted drug delivery and theranostics have indisputable advantages over other nanoparticles.