Lipid core nanoparticles as a broad strategy to reverse fluconazole resistance in multiple Candida species.
Colloids Surf B Biointerfaces
; 175: 523-529, 2019 Mar 01.
Article
in En
| MEDLINE
| ID: mdl-30579053
ABSTRACT
Fungal resistance is the major problem related to fluconazole treatments. This study aims to develop innovative lipid core nanocapsules and nanostructured lipid carriers containing fluconazole, to study in vitro antifungal activity and to assess the possibility of resistance reversion in Candida albicans, C. glabrata, C. krusei, and C. tropicalis isolates. The action mechanism of nanoparticles was investigated through efflux pumps and scanning electron microscopy studies. The lipid core nanocapsules and nanostructured lipid carriers were prepared by interfacial deposition of preformed polymer and high-pressure homogenization methods, respectively. Both nanostructures presented sizes below 250 nm, SPAN < 1.6, negative zeta potential, pH slightly acid, high drug content and controlled drug release. The nanostructured lipid carriers were unable to reverse the fungal resistance. Lipid core nanoparticles displayed advantages such as a reduction in the effective dose of fluconazole and resistance reversion in all isolates tested - with multiple mechanisms of resistance. The main role of the supramolecular structure and the composition of the nanoparticles on antifungal mechanisms of action were discussed. The results achieved through this study have an impact on clinical therapy, with a potential application in the treatment of fungal infections caused by resistant isolates of Candida spp.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Candida
/
Fungal Proteins
/
Fluconazole
/
Drug Resistance, Fungal
/
Delayed-Action Preparations
/
Nanoparticles
/
Antifungal Agents
Language:
En
Journal:
Colloids Surf B Biointerfaces
Journal subject:
QUIMICA
Year:
2019
Document type:
Article
Affiliation country:
Brazil