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Self-organized nanoparticles based on drug-interpolyelectrolyte complexes as drug carriers

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Abstract

Potential applications in drug delivery from nanostructures composed of two oppositely charged polymethacrylates, eudragit® L100 (EL) and eudragit® EPO (EE), loaded with three model basic drugs (D), atenolol, propranolol, and metroclopramide were evaluated. The self-organized nanoparticles based on drug-interpolyelectrolyte complexes (DIPEC), (EL-D50)–EEX, were obtained by mixing the aqueous dispersions of both polyelectrolytes at room temperature in an ultrasound bath. Dispersions of (EL-D50) neutralized with increasing proportions of EE exhibited a rise of turbidity, particle sizes in the range of 150–400 nm, and high negative zeta potential. The sign of zeta potential was shifted from negative to positive by changes in composition of DIPEC. Freeze dried DIPEC were easily redispersed in water yielding nearly the same parameters of fresh dispersions. In vitro release experiments using Franz cells showed that DIPEC systems behave as a drug reservoir that slowly releases the drug as water is placed in the receptor compartment. The release rate was raised by ionic exchange with counterions present in simulated physiological fluids placed in the receptor media. Delivery of D from DIPEC exhibited a remarkable robustness toward simulated physiological media of different pH. The DIPEC systems exhibit interesting properties to design nanoparticulate drug delivery systems for oral and/or topical routes.

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Acknowledgments

Financial supports from the National Council of Scientific and Technological Research CONICET, FONCyT PICT-2008-1476 and the National University of Córdoba (SECyT-UNC), Córdoba, Argentina are greatly acknowledged. M.C. Palena thanks CONICET for research fellowships. The authors would like to thank Etilfarma® S.A. (Buenos Aires, Arg.) for the provision of Eudragit® (L100 and EPO). The authors wish to thank: Prof. M.E. Olivera for the manuscript revision, Center of Metrology-CEMETRO, Universidad Tecnologica Nacional, Facultad Regional Córdoba and Dr. Daniel Brusa, who kindly performed the AFM images.

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  1. Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, UNITEFA-CONICET, Edificio Ciencias 2, Ciudad Universitaria, X5000HUA, Córdoba, Argentina

    M. C. Palena, R. H. Manzo & A. F. Jimenez-Kairuz

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  1. M. C. Palena
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  2. R. H. Manzo
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  3. A. F. Jimenez-Kairuz
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Correspondence to A. F. Jimenez-Kairuz.

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Palena, M.C., Manzo, R.H. & Jimenez-Kairuz, A.F. Self-organized nanoparticles based on drug-interpolyelectrolyte complexes as drug carriers. J Nanopart Res 14, 867 (2012). https://doi.org/10.1007/s11051-012-0867-8

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