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Compared to conventional therapeutics, nano-drugs have to manifest higher stability and circulation time, reduced toxicity and improved targeted delivery. Despite the obvious benefit, the accumulation of imaging agents and nano-carriers in the body following their therapeutic or diagnostic application generates concerns about their short, medium and long term safety for human health. Numerous toxicology studies have demonstrated that exposure to nanomaterials (NMs) might pose serious risks to humans. Epigenetic modifications, representing a non-genotoxic mechanism of toxicant-induced health effects, are becoming recognized as playing a potential causative role in the etiology of many diseases including cancer.