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Antimalarial Activity of Orally Administered Curcumin Incorporated in Eudragit®-Containing Liposomes

1
Nanomalaria Group, Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute of Science and Technology, Baldiri Reixac 10-12, ES-08028 Barcelona, Spain
2
Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-Universitat de Barcelona), Rosselló 149-153, ES-08036 Barcelona, Spain
3
Nanoscience and Nanotechnology Institute (IN2UB), University of Barcelona, Martí i Franquès 1, ES-08028 Barcelona, Spain
4
Department of Scienze della Vita e dell’Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2018, 19(5), 1361; https://doi.org/10.3390/ijms19051361
Received: 22 February 2018 / Revised: 18 April 2018 / Accepted: 27 April 2018 / Published: 4 May 2018
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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Abstract

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. View Full-Text
Keywords: malaria; curcumin; nanomedicine; oral administration; lipid nanovesicles; Eudragit; Nutriose; hyaluronan; Plasmodium yoelii malaria; curcumin; nanomedicine; oral administration; lipid nanovesicles; Eudragit; Nutriose; hyaluronan; Plasmodium yoelii
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Martí Coma-Cros, E.; Biosca, A.; Lantero, E.; Manca, M.L.; Caddeo, C.; Gutiérrez, L.; Ramírez, M.; Borgheti-Cardoso, L.N.; Manconi, M.; Fernàndez-Busquets, X. Antimalarial Activity of Orally Administered Curcumin Incorporated in Eudragit®-Containing Liposomes. Int. J. Mol. Sci. 2018, 19, 1361.

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