Recently, nanotechnology became an integral part of drug design especially in the area of targeted drug delivery. The nanoparticles are characterized by the ability to target deep tissues, easily surface decoration, controlling the drug release, ease of detection and follow up, high stability and good biocompatibility. Gold nanoparticles represent very important class of nanoparticles and it is expected to have great impact on drug development. The intention of this manuscript is to address the most recent medicinal application of gold nanoparticles especially in the area of targeted drug delivery. This manuscript will be very helpful for academic, students, pharmaceutical companies and peoples working in targeted drug delivery.