Gold nanoparticles (GNPs) have generated keen interest among researchers in recent years due to their excellent physicochemical properties. In general, GNPs are biocompatible, amenable to desired functionalization, non-corroding, and exhibit size and shape dependent optical and electronic properties. These excellent properties of GNPs exhibit their tremendous potential for use in diverse biomedical applications. Herein, we have evaluated the recent advancements of GNPs to highlight their exceptional potential in the biomedical field. Special focus has been given to emerging biomedical applications including bio-imaging, site specific drug/gene delivery, nano-sensing, diagnostics, photon induced therapeutics, and theranostics. We have also elaborated on the basics, presented a historical preview, and discussed the synthesis strategies, functionalization methods, stabilization techniques, and key properties of GNPs. Lastly, we have concluded this article with key findings and unaddressed challenges. Overall, this review is a complete package to understand the importance and achievements of GNPs in the biomedical field.