In vitro antifungal activity and toxicity of itraconazole in DMSA-PLGA nanoparticles

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...

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Bibliographic Details
Published inJournal of nanoscience and nanotechnology Vol. 11; no. 3; p. 2308
Main Authors Cunha-Azevedo, Elaine P, Silva, Jaqueline R, Martins, Olimpia P, Siqueira-Moura, Marigilson P, Bocca, Anamélia L, Felipe, Maria Sueli S, Tedesco, Antonio C, Azevedo, Ricardo B
Format Journal Article
LanguageEnglish
Published United States 01.03.2011
Subjects
Animals
Antifungal Agents - administration & dosage
Antifungal Agents - chemistry
Antifungal Agents - toxicity
Cell Line
Cell Survival - drug effects
Dose-Response Relationship, Drug
Humans
Itraconazole - administration & dosage
Itraconazole - chemistry
Itraconazole - toxicity
Lactic Acid - chemistry
Mice
Nanocapsules - chemistry
Nanocapsules - ultrastructure
Paracoccidioides - cytology
Paracoccidioides - drug effects
Polyglycolic Acid - chemistry
Polylactic Acid-Polyglycolic Acid Copolymer
Succimer - chemistry
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Summary: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).
ISSN:1533-4880
DOI:10.1166/jnn.2011.3576