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

Molecules

Pedro Pires Goulart Guimar฾s²  Sheila Rodrigues Oliveira²  Gabrielle de Castro Rodrigues²  Savio Morato Lacerda Gontijo¹  Ivana Silva Lula²  Maria Esperanza Cortés¹  Ângelo Márcio Leite Denadai³  Rubén Dario Sinisterra² 

[1] Department of Restorative Dentistry, Faculty of Dentistry, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil; E-Mails:;Chemistry Department, Institute of Exact Sciences, Universidade Federal de Minas Gerais, Av. Antonio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte-MG, Brazil; E-Mails:;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; E-Mail:

关键词: 5-FU;    PLGA;    antitumor nanoparticles;    sulfadiazine;    drug delivery;   

DOI  :  10.3390/molecules20010879

来源: mdpi

【 摘 要 】

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, D_h = 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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.