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Antioxidants have been found to be effective as prophylatic and therapeutic agents for different diseases such as diabetes, cancer, and neurodegenerative disorders. However, antioxidant substances can present poor solubility in water, inefficient permeability, gastrointestinal degradation, first-pass effect, and/or instability during storage. These drawbacks can be potentially circumvented by encapsulating the susceptible antioxidants. Polymeric nanoparticles (nanocapsules or nanospheres) have been used to improve the drug efficacy and release. Our group has shown that the in vitro antioxidant effect of melatonin against lipid peroxidation in microsomes and liposomes can be improved by encapsulation of the antioxidant drug in polymeric nanoparticles.