Discovering the vast therapeutic potential of siRNA opened up new clinical research areas focussing on a number of diseases and applications; however significant problems with siRNA stability and delivery have hindered its clinical applicability. As a result, interest in the development of practical siRNA delivery systems has grown in recent years. Of the numerous siRNA delivery strategies currently on offer, gold nanoparticles (AuNPs) stand out thanks to their biocompatibility and capacity to protect siRNA against degradation; not to mention the versatility offered by their tuneable shape, size and optical properties. Herein this review provides a complete summary of the methodologies for functionalizing AuNPs with siRNA, paying singular attention to the AuNP shape, size and surface coating, since these key factors heavily influence cellular interaction, internalization and, ultimately, the efficacy of the hybrid particle. The most noteworthy hybridization strategies have been highlighted along with the most innovative and outstanding in vivo studies with a view to increasing clinical interest in the use of AuNPs as siRNA nanocarriers.