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Self-Assembled Benznidazole-Loaded Cationic Nanoparticles Containing Cholesterol/Sialic Acid: Physicochemical Properties, In Vitro Drug Release and In Vitro Anticancer Efficacy

1
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
2
Department of Morphology, Federal University of Rio Grande do Norte, UFRN, Natal 59078-970, Brazil
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(9), 2350; https://doi.org/10.3390/ijms20092350
Received: 26 February 2019 / Revised: 8 April 2019 / Accepted: 10 April 2019 / Published: 11 May 2019
(This article belongs to the Special Issue Surface-Functionalized Nanoparticles as Drug Carriers)
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Abstract

Cationic polymeric nanoparticles (NPs) have the ability to overcome biological membranes, leading to improved efficacy of anticancer drugs. The modulation of the particle-cell interaction is desired to control this effect and avoid toxicity to normal cells. In this study, we explored the surface functionalization of cationic polymethylmethacrylate (PMMA) NPs with two natural compounds, sialic acid (SA) and cholesterol (Chol). The performance of benznidazole (BNZ) was assessed in vitro in the normal renal cell line (HEK-293) and three human cancer cell lines, as follows: human colorectal cancer (HT-29), human cervical carcinoma (HeLa), and human hepatocyte carcinoma (HepG2). The structural properties and feasibility of NPs were evaluated and the changes induced by SA and Chol were determined by using multiple analytical approaches. Small (<200 nm) spherical NPs, with a narrow size distribution and high drug-loading efficiency were prepared by using a simple and reproducible emulsification solvent evaporation method. The drug interactions in the different self-assembled NPs were assessed by using Fourier transform-infrared spectroscopy. All formulations exhibited a slow drug-release profile and physical stability for more than 6 weeks. Both SA and Chol changed the kinetic properties of NPs and the anticancer efficacy. The feasibility and potential of SA/Chol-functionalized NPs has been demonstrated in vitro in the HEK-293, HepG2, HeLa, and HT-29 cell lines as a promising system for the delivery of BNZ. View Full-Text
Keywords: functionalization of nanoparticles; surface of nanoparticles; structural properties; cationic nanoparticles; biodegradable nanoparticles functionalization of nanoparticles; surface of nanoparticles; structural properties; cationic nanoparticles; biodegradable nanoparticles
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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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dos Santos-Silva, A.M.; de Caland, L.B.; do Nascimento, E.G.; Oliveira, A.L.C.S.; de Araújo-Júnior, R.F.; Cornélio, A.M.; Fernandes-Pedrosa, M.F.; da Silva-Júnior, A.A. Self-Assembled Benznidazole-Loaded Cationic Nanoparticles Containing Cholesterol/Sialic Acid: Physicochemical Properties, In Vitro Drug Release and In Vitro Anticancer Efficacy. Int. J. Mol. Sci. 2019, 20, 2350.

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