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Gold NPs have great potential in biomedical applications. PAMAM dendrimers are spherical, hyper branched macromolecules which can encapsulate therapeutic molecules while stabilizing metal nanoparticle such as gold NPs. The aim of the current study was to investigate the theranostic capability of curcumin-loaded dendrimer-gold hybrid structure.Dendrimer-gold hybrid structure was synthesized by complexing AuCl4− ions with PEGylated amine-terminated generation 5 poly (amidoamine) dendrimer. The resultant hybrid system was loaded with curcumin. The curcumin-loaded PEGylated Au dendrimer was further conjugated to MUC-1 aptamer in order to target the colorectal adenocarcinoma in vitro and in vivo.Obtained results demonstrated that the targeted theranostic agent was accumulated in HT29 and C26 cells in vitro and showed higher cellular cytotoxicity in comparison with non-targeted system. On the other hand, in vivo experiment demonstrated the potential of targeted theranostic system in CT-scan tumor imaging as well as cancer therapy.Findings from this study suggested that MUC-1 targeted curcumin-loaded PEGylated Au dendrimers have good X-ray attenuation and is desirable probe for CT imaging while demonstrating high therapeutic index against colorectal cancer adenocarcinoma.