Arias J. L. auteur aut IRD Cebrian-Torrejon G. auteur aut IRD Poupon E. auteur aut IRD Fournet Alain auteur aut IRD Couvreur P. auteur aut IRD text journalArticle eng text/pdf born digital access The efficacy of antiprotozoal agents against intracellular infections is very often limited by an almost negligible access to the cellular level where the pathogens are hidden. As a result, high doses of the chemotherapy agents are needed to be administered, but the great incidence of severe adverse drug effects generally leads to pharmacotherapy failure. To enhance the pharmacological effect of the antiprotozoal and antifungal canthin-6-one, loading into biodegradable poly(octylcyanoacrylate) nanoparticles has been considered. The preparation of canthin-6-one nanoformulation (average size a parts per thousand 170 nm) has been performed by a single-absorption procedure with high drug loading and little burst release as determined by RP-HPLC. Further characterization of this nanoformulation has been carry out by electrophoretic measurements, analysis of the surface thermodynamics of the nanoparticles, and (1)H-NMR analysis. Nanoparticles loaded with canthin-6-one were characterized by a significant hydrophobicity and a great surface electrical charge under physiological conditions. These are two key physicochemical factors determining recognition by the reticuloendothelial system, resulting in a fast intracellular uptake by infected phagocytes. It is expected that this nanoformulation offers potential applications for an efficient canthin-6-one delivery to intracellular infections. specialized Canthin-6-one Drug delivery Intracellular infection Nanoformulation Poly(octylcyanoacrylate) Reticuloendothelial system 020 13 12 6737-6746 2011 1388-0764 https://www.documentation.ird.fr/hor/fdi:010054289 10.1007/s11051-011-0580-z 1388-0764 [F B010054289] https://www.documentation.ird.fr/hor/fdi:010054289 https://www.documentation.ird.fr/intranet/publi/2012/01/010054289.pdf Accès réservé (Intranet de l'IRD) IRD - Base Horizon / Pleins textes 2012-02-01 2017-08-23 fdi:010054289 fre