Nanoformulation of curcumin-loaded eudragit-nutriosomes to counteract malaria infection by a dual strategy: Improving antioxidant intestinal activity and systemic efficacy

In this paper, nutriosomes (phospholipid vesicles associated with Nutriose (R) FM06) were modified to obtain new systems aimed at enhancing the efficacy of curcumin in counteracting malaria infection upon oral administration. Eudragit (R) L100, a pH-sensitive co-polymer, was added to these vesicles, thus obtaining eudragit-nutriosomes, to improve their in vivo performances. Liposomes without eudragit and nutriose were also prepared as a reference. Cryo-TEM images showed the formation of multicompartment vesicles, with mean diameter around 300 nm and highly negative zeta potential. Vesicles were stable in fluids mimicking the gastro-intestinal content due to the high phospholipid concentration and the presence of gastro-resistant eudragit and digestion-resistant nutriose. Eudragit-nutriosomes disclosed promising performances in vitro and in vivo: they maximized the ability of curcumin to counteract oxidative stress in intestinal cells (Caco-2), which presumably reinforced its systemic efficacy. Orally-administered curcumin-loaded eudragit-nutriosomes increased significantly the survival of malaria-infected mice relative to free curcumin-treated controls.