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J Nanosci Nanotechnol ; 11(3): 2308-14, 2011 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21449386

RESUMO

Itraconazole (ITZ) is a drug used to treat various fungal infections and may cause side effects. The aim of this study was to develop and evaluate the in vitro activity of DMSA-PLGA nanoparticles loaded with ITZ against Paracoccidioides brasiliensis, as well as their cytotoxicity. Nanoparticles were prepared using the emulsification-evaporation technique and characterized by their encapsulation efficiency, morphology (TEM), size (Nanosight) and charge (zeta potential). Antifungal efficacy in P. brasiliensis was determined by minimal inhibition concentration (MIC), and cytotoxicity using MTT assay. ITZ was effectively incorporated in the PLGA-DMSA nanoparticles with a loading efficiency of 72.8 +/- 3.50%. The shape was round with a solid polymeric structure, and a size distribution of 174 +/- 86 nm (Average +/- SD). The particles were negatively charged. ITZ-NANO presented antifungal inhibition (MIC = 6.25 ug/mL) against P. brasiliensis and showed lower in vitro cytotoxicity than free drug (ITZ).


Assuntos
Sobrevivência Celular/efeitos dos fármacos , Itraconazol/administração & dosagem , Itraconazol/toxicidade , Ácido Láctico/química , Nanocápsulas/química , Paracoccidioides/efeitos dos fármacos , Ácido Poliglicólico/química , Succímero/química , Animais , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/toxicidade , Linhagem Celular , Relação Dose-Resposta a Droga , Humanos , Itraconazol/química , Camundongos , Nanocápsulas/ultraestrutura , Paracoccidioides/citologia , Copolímero de Ácido Poliláctico e Ácido Poliglicólico
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