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Objective (s): Several studies reported the apoptotic and lytic activity of melittin (Mel) in different tumor cells. In this study, a novel nano-complex was developed composed of AS1411aptamers, melittin and gold nanoparticle for the treatment of breast cancer cells.

Materials and Methods: Gold nanoparticles (GNP) were synthesized using reduction of tetrachloroauric acid (HAuCl4). Melittin modified with cysteine and AS1411aptamer conjugated to the gold nanoparticle. Gel retardation assay was used to prove the formation of GNP-Mel-AS1411 complex. Physicochemical properties of complex were investigated by Dynamic Light Scattering (DLS). The cytotoxicity of Mel and GNP-Mel-AS1411 complex were evaluated in both MCF‐7 (target) and L929 (non-target) cells by the MTT assay. Results: The average size of GNP and GNP-Mel-AS1411 complex were 20±2.5 and 270.5±3.2 respectively. The results of MTT assay revealed that this nanocomplex was more cytotoxic in MCF‐7 (cell viability= 19%±2%) and less cytotoxic in L929 cells (cell viability= 73%±1.6%). Conclusion: The results of this study indicated that the gold nanoparticle-melittin-AS1411 complex had a potential value in cancer cell targeted delivery of melittin.