Nanopartículas de quitosana e carragenanas: produção, caracterização e avaliação preliminar como sistema de liberação controlada de 5-fluorouracil

• Ano de defesa: 2013
• Autor(a) principal: Chaves, Luciano de Sousa
• Tipo de documento: Tese
• Tipo de acesso: Acesso aberto
• Idioma: por
• Palavras-chave em Português: Bioquímica; Nanopartículas; Quitosana; Carragenana; Atividade antitumoral; Liberação de fármacos
• Link de acesso: http://www.repositorio.ufc.br/handle/riufc/18832

The nanoparticle drug delivery systems are a promising strategy to avoid the adverse conventional effects of cancer chemotherapy. In this work, nanoparticles produced by polyelectrolytic complexation of chitosan and κ, ι, λ-carrageenan were evalueted as a release system of 5-Fluorouracil. At first, the polyelectrolyte complexes were produced from several experimental conditions such as initial polyelectrolytes concentration (0.5, 0.25 and 0.1), charge ratio (10, 1 and 0.1) and mixing order of the polyelectrolytes solutions. The complexes presented hydrodynamic diameter (Dh) between 217 and 1,555 nm, with polydispersity indexes (PDI) below 0.6. The complexes showed zeta potential above 30 mV for cationic particles and below -30 mV for anionic particles, indicating that the complexes have high stability. The nanoparticles showed soft size, polydispersity index and zeta potential variation during 30 days of storage. The Fourier transform infrared spectroscopy (FTIR) proved the interaction of the amine groups of chitosan and sulfate groups of carrageenan in the nanoparticles formation. The 5-FU entrapment in the nanoparticles was also confirmed by FTIR and promoted soft changes on characteristics of the complexes. The encapsulation efficiency ranged from 3.5 ± 1.1 to 15.4 ± 0.6%, the load capacity was maintained between 8.2 ± 0.4 and 38 ± 2.4%, and both were affected by 5-FU initial concentration. The in vitro drug release assay showed a burst effect with much of the drug being released within the first hours, followed by a slow and incomplete release over 8 hours of the experiment. The nanoparticles/5-FU complex showed low cytotoxic effect on tumor cell lines HL-60 and HCT-116, probably due to slightly alkaline pH of the culture medium. This result indicates the need for evaluating in vivo models to study the chitosan/carrageenan/5-FU nanoparticles as a promising tumor targeting delivery system.