Programa de Pós-Graduação em Ciências Farmacêuticas
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Doctoral Thesis Nanopartículas biodegradáveis e biocompatíveis para liberação modificada de benznidazol(2019-06-27) Silva, Alaine Maria dos Santos; Silva Júnior, Arnóbio Antonio da; ; ; Silva, Marcelo de Sousa da; ; Damasceno, Bolivar Ponciano Goulart de Lima; ; Porto, Carlos Alberto Robello; ; Soares Sobrinho, José Lamartine;Benznidazole (BNZ) is the drug of choice for the treatment of patients with infection by Trypanosoma cruzi. Despite its wide use, this molecule presents efficacy problems due to high toxicity, in addition to low solubility in aqueous medium. The nanoparticles have proven ability to traverse most biological barriers and intracellular targeting of drugs, especially when surface binders are inserted to increase the efficacy of the drug in cells infected. The aim of this work was to make a structural design and monitoring of functionalized and fluorescent nanoparticles of poly (lactic-co-glycolic acid) (PLGA) for modified release of benznidazole. The particles were produced by the emulsification solvent evaporation method. The development of the formulation and parameters of obtaining were optimized by measurements of particle size, polydispersity index, zeta potential, atomic force microscopy (MFA), scanning electron microscopy (SEM), confocal microscopy (MC), fourier transform infrared absorption spectroscopy (FTIRATR), encapsulation efficiency, in vitro and in vivo studies. Spherical and stables polymeric nanoparticles below 250 nm were obtained, with encapsulation efficiency greater than 95%. The in vitro release kinetics of the drug showed a slow release of the drug and the improvement of the biological activity of nanoparticles containing BNZ. In vitro assays in normal cells (Hek 293), tumor cells (Hep G2 and HT-29), amastigotes (strains H9c2 and Dm28c) and with epimastigotes (strains Y, CL-Brenner and Dm28c) showed an increase in the potency of the nanoparticles containing BNZ over the free BNZ. The confocal microscopy analysis showed that the nanoparticles come in the parasite with high efficiency, especially those functionalized with sialic acid and cholesterol. In vivo tests revealed that the nanoparticles containing BNZ had similar effect to the free BNZ, even used in 20-fold inferior concentration. Thus, the present work systematically discusses the development of a nanotechnological system with innovative potential to increase the efficacy of benznidazole in cells infected with Trypanosoma cruzi.Master Thesis Nanopartículas catiônicas obtidas por emulsificação com evaporação de solvente para liberação modificada benznidazol(2015-07-02) Silva, Alaine Maria dos Santos; Silva Júnior, Arnobio Antonio da; ; ; Caroni, Ana Luiza Porpino Fernandes; ; Reynaud, Franceline;