Cancer is a major cause of deaths. More recently, drug delivery systems (DDSs) using gold nanoparticles (GNPs) have been widely developed in cancer therapy for their easily synthesised, functionalised, better biocompatible, and low toxicity properties. Gold nanoparticle–based platforms as cancer–targeted molecules delivery to tumour tissues have been proposed as an effective strategy by overcoming various biological barriers and increasing retention effect. Coupled with the active targeting on the specific sites during cancer process they can facilitate anticancer effects. This review is focused on the current applications of GNPs as improving cancer–targeted delivery platforms.