Functionalized gold nanoparticles are being used extensively for many biomedical applications and research has shown an abundant use in targeted delivery. AuNPs are small gold particles that have a diameter between 1nm to 100nm. More lately, these unique optoelectronic properties have been researched and employed in high technology applications like organic photovoltaics, sensory probes, therapeutic agents, drug delivery in biological and medical applications, electronic conductors and catalysis. The optical and electronic properties of gold nanoparticles are tunable by altering the size, shape, surface chemistry, or aggregation state. This review will provide a comprehensive review of recent advances and future perspectives of AuNp’s in targeted therapy and diagnostics.