by Keyword: Oral administration

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Manconi, M., Manca, M. L., Escribano-Ferrer, E., Coma-Cros, E. M., Biosca, A., Lantero, E., Fernàndez-Busquets, X., Fadda, A. M., Caddeo, C., (2019). Nanoformulation of curcumin-loaded eudragit-nutriosomes to counteract malaria infection by a dual strategy: Improving antioxidant intestinal activity and systemic efficacy International Journal of Pharmaceutics 556, 82-88

In this paper, nutriosomes (phospholipid vesicles associated with Nutriose® FM06) were modified to obtain new systems aimed at enhancing the efficacy of curcumin in counteracting malaria infection upon oral administration. Eudragit® 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.

Keywords: Eudragit® L100, Nutriose® FM06, Nutriosomes, Curcumin, Oral administration, Malaria

Martí Coma-Cros, Elisabet, Biosca, Arnau, Lantero, Elena, Manca, Maria, Caddeo, Carla, Gutiérrez, Lucía, Ramírez, Miriam, Borgheti-Cardoso, Livia, Manconi, Maria, Fernàndez-Busquets, Xavier, (2018). Antimalarial activity of orally administered curcumin incorporated in Eudragit®-containing liposomes International Journal of Molecular Sciences , 19, (5), 1361

Curcumin is an antimalarial compound easy to obtain and inexpensive, having shown little toxicity across a diverse population. However, the clinical use of this interesting polyphenol has been hampered by its poor oral absorption, extremely low aqueous solubility and rapid metabolism. In this study, we have used the anionic copolymer Eudragit® S100 to assemble liposomes incorporating curcumin and containing either hyaluronan (Eudragit-hyaluronan liposomes) or the water-soluble dextrin Nutriose® FM06 (Eudragit-nutriosomes). Upon oral administration of the rehydrated freeze-dried nanosystems administered at 25/75 mg curcumin·kg−1·day−1, only Eudragit-nutriosomes improved the in vivo antimalarial activity of curcumin in a dose-dependent manner, by enhancing the survival of all Plasmodium yoelii-infected mice up to 11/11 days, as compared to 6/7 days upon administration of an equal dose of the free compound. On the other hand, animals treated with curcumin incorporated in Eudragit-hyaluronan liposomes did not live longer than the controls, a result consistent with the lower stability of this formulation after reconstitution. Polymer-lipid nanovesicles hold promise for their development into systems for the oral delivery of curcumin-based antimalarial therapies.

Keywords: Malaria, Curcumin, Nanomedicine, Oral administration, Lipid nanovesicles, Eudragit, Nutriose, Hyaluronan, Plasmodium yoelii