title: Development of sulfadiazine-decorated PLGA nanoparticles loaded with 5-fluorouracil and cell viability.
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.
authors.affiliation: Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. pedropiresg@ufmg.br.
authors.forename: Pedro Pires Goulart
authors.initials: PP
authors.lastname: Guimarães
authors.affiliation: Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. shetq@yahoo.com.br.
authors.forename: Sheila Rodrigues
authors.initials: SR
authors.lastname: Oliveira
authors.affiliation: Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. gabrielledecastro@hotmail.com.
authors.forename: Gabrielle
authors.initials: G
authors.lastname: de Castro Rodrigues
authors.affiliation: Department of Restorative Dentistry, Faculty of Dentistry, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. savio.morato@yahoo.com.br.
authors.forename: Savio Morato Lacerda
authors.initials: SM
authors.lastname: Gontijo
authors.affiliation: Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. ivanalula@ufmg.br.
authors.forename: Ivana Silva
authors.initials: IS
authors.lastname: Lula
authors.affiliation: Department of Restorative Dentistry, Faculty of Dentistry, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. mecortes@yahoo.com.
authors.forename: Maria Esperanza
authors.initials: ME
authors.lastname: Cortés
authors.affiliation: 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. angelo.denadai@ufjf.edu.br.
authors.forename: Ângelo Márcio Leite
authors.initials: ÂM
authors.lastname: Denadai
authors.affiliation: Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil. sinisterra@ufmg.br.
authors.forename: Rubén Dario
authors.initials: RD
authors.lastname: Sinisterra
mesh_terms: D002152:Calorimetry, Differential Scanning; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D005472:Fluorouracil / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D055672:Static Electricity; D013411:Sulfadiazine / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013411:Sulfadiazine; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D005472:Fluorouracil