The objective of the present study was to evaluate the oral toxicity of chitosan reduced gold nanoparticles so as to demonstrate its applicability for drug delivery application. Acute oral toxicity studies in female rats documented no deaths or treatment related complications. The LD(50) value of gold nanoparticles was found to be greater than 2000 mg/kg. In case of sub-acute oral toxicity studies, gold nanoparticles were administered orally to male and female rats for a period of 28-days. At the end of study blood samples were collected for haematology and biochemical analysis. For histopathological analysis, organs of animals were weighed and processed for examination. All animals survived the duration of the study, with no significant changes in clinical signs, body weight, food consumption, hematological parameters, organ weights and histopathological findings. These studies establish that chitosan reduced gold nanoparticles produced no treatment related toxicity in rats following oral administration, thus can be exploited for potential therapeutic applications.