title: In vitro antifungal activity and toxicity of itraconazole in DMSA-PLGA nanoparticles.
abstract: 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).
authors: Biological Sciences Institute, Universidade de Brasília, Brasília DF 70910-900, Brazil.
authors: Elaine P
authors: EP
authors: Cunha-Azevedo
authors: Jaqueline R
authors: JR
authors: Silva
authors: Olimpia P
authors: OP
authors: Martins
authors: Marigilson P
authors: MP
authors: Siqueira-Moura
authors: Anamélia L
authors: AL
authors: Bocca
authors: Maria Sueli S
authors: MS
authors: Felipe
authors: Antonio C
authors: AC
authors: Tedesco
authors: Ricardo B
authors: RB
authors: Azevedo
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D017964:Itraconazole / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity*; D019344:Lactic Acid / Q000737:chemistry*; D051379:Mice; D053769:Nanocapsules / Q000737:chemistry* / Q000648:ultrastructure; D010228:Paracoccidioides / Q000166:cytology / Q000187:drug effects*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D004113:Succimer / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D053769:Nanocapsules; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D017964:Itraconazole; D019344:Lactic Acid; D004113:Succimer