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Molecules 2015, 20(1), 879-899; doi:10.3390/molecules20010879

Development of Sulfadiazine-Decorated PLGA Nanoparticles Loaded with 5-Fluorouracil and Cell Viability

1
Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil
2
Department of Restorative Dentistry, Faculty of Dentistry, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil
3
Pharmaceutical Department, Universidade Federal de Juiz de Fora, Campus Governador Valadares-MG, Av. Dr. Raimundo Monteiro de Rezende, 330, Centro, CEP 35010-177 Governador Valadares-MG, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 24 October 2014 / Accepted: 29 December 2014 / Published: 8 January 2015
(This article belongs to the Section Medicinal Chemistry)
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Abstract

The aim of this work was to synthesize sulfadiazine-poly(lactide-co-glycolide) (SUL-PLGA) nanoparticles (NPs) for the efficient delivery of 5-fluorouracil to cancer cells. The SUL-PLGA conjugation was assessed using FTIR, 1H-NMR, 13C-NMR, elemental analysis and TG and DTA analysis. The SUL-PLGA NPs were characterized using transmission and scanning electron microscopy and dynamic light scattering. Additionally, the zeta potential, drug content, and in vitro 5-FU release were evaluated. We found that for the SUL-PLGA NPs, Dh = 114.0 nm, ZP = −32.1 mV and the encapsulation efficiency was 49%. The 5-FU was released for up to 7 days from the NPs. Cytotoxicity evaluations of 5-FU-loaded NPs (5-FU-SUL-PLGA and 5-FU-PLGA) on two cancer cell lines (Caco-2, A431) and two normal cell lines (fibroblast, osteoblast) were compared. Higher cytotoxicity of 5-FU-SUL-PLGA NPs were found to both cancer cell lines when compared to normal cell lines, demonstrating that the presence of SUL could significantly enhance the cytotoxicity of the 5-FU-SUL-PLGA NPs when compared with 5-FU-PLGA NPs. Thus, the development of 5-FU-SUL-PLGA NPs to cancer cells is a promising strategy for the 5-FU antitumor formulation in the future. View Full-Text
Keywords: 5-FU; PLGA; antitumor nanoparticles; sulfadiazine; drug delivery 5-FU; PLGA; antitumor nanoparticles; sulfadiazine; drug delivery
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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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MDPI and ACS Style

Guimarães, P.P.G.; Oliveira, S.R.; de Castro Rodrigues, G.; Gontijo, S.M.L.; Lula, I.S.; Cortés, M.E.; Denadai, Â.M.L.; Sinisterra, R.D. Development of Sulfadiazine-Decorated PLGA Nanoparticles Loaded with 5-Fluorouracil and Cell Viability. Molecules 2015, 20, 879-899.

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