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Int J Mol Sci. 2019 May 11;20(9). pii: E2350. doi: 10.3390/ijms20092350.

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

Author information

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. alaine.maria@hotmail.com.
2
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. liliabasiliocaland@gmail.com.
3
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. ednaldogn40@gmail.com.
4
Department of Morphology, Federal University of Rio Grande do Norte, UFRN, Natal 59078-970, Brazil. analu.cs@hotmail.com.
5
Department of Morphology, Federal University of Rio Grande do Norte, UFRN, Natal 59078-970, Brazil. araujojr@cb.ufrn.br.
6
Department of Morphology, Federal University of Rio Grande do Norte, UFRN, Natal 59078-970, Brazil. alianda@neuro.ufrn.br.
7
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. mffpedrosa@gmail.com.
8
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. arnobiosilva@gmail.com.

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.

KEYWORDS:

biodegradable nanoparticles; cationic nanoparticles; functionalization of nanoparticles; structural properties; surface of nanoparticles

PMID:
31083590
PMCID:
PMC6539689
DOI:
10.3390/ijms20092350
[Indexed for MEDLINE]
Free PMC Article

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