Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)

Nicolás Gómez-Sequeda,1 Rodrigo Torres,2 Claudia Ortiz3 1School of Biology, 2School of Chemistry, Faculty of Sciences, 3School of Microbiology, Faculty of Health, Universidad Industrial de Santander, Bucaramanga, Santander, Colombia Abstract: In this study, nanoparticles (NPs)...

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Autores principales: Gómez-Sequeda N, Torres R, Ortiz C
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Publicado: Dove Medical Press 2017
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spelling oai:doaj.org-article:8b23f649301a4073a2004c8cdbab9a162021-12-02T04:04:20ZSynthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)1177-8903https://doaj.org/article/8b23f649301a4073a2004c8cdbab9a162017-05-01T00:00:00Zhttps://www.dovepress.com/synthesis-characterization-and-in-vitro-activity-against-candida-spp-o-peer-reviewed-article-NSAhttps://doaj.org/toc/1177-8903Nicolás Gómez-Sequeda,1 Rodrigo Torres,2 Claudia Ortiz3 1School of Biology, 2School of Chemistry, Faculty of Sciences, 3School of Microbiology, Faculty of Health, Universidad Industrial de Santander, Bucaramanga, Santander, Colombia Abstract: In this study, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) loaded with fluconazole (FLZ) and FLZ-NPs coated with the cationic polymer polyethylenimine (PEI) (FLZ-NP-PEI) were synthetized in order to improve antimycotic activity against four strains of Candida spp. of clinical relevance. FLZ-NPs and FLZ-NP-PEI were synthesized by double emulsion solvent-diffusion (DES-D) and characterized. Minimum inhibitory concentration (MIC50) and minimum fungicide concentration (MFC) were determined in vitro by culturing Candida strains in the presence of these nanocompounds. FLZ-NPs were spherical in shape with hydrodynamic sizes of ~222 nm and surface charge of -11.6 mV. The surface charges of these NPs were successfully modified using PEI (FLZ-NP-PEI) with mean hydrodynamic sizes of 281 nm and surface charge of 23.5 mV. The efficiency of encapsulation (~53%) and a quick release of FLZ (≥90% after 3 h) were obtained. Cytotoxicity assay showed a good cell viability for FLZ-NPs (≥86%), and PEI-modified NPs presented a decrease in cell viability (~38%). FLZ-NPs showed an increasing antifungal activity of FLZ for sensitive (Candida parapsilosis ATCC22019 and Candida albicans ATCC10231, MIC50 =0.5 and 0.1 µg/mL, respectively) and resistant strains (Candida glabrata EMLM14 and Candida krusei ATCC6258, MIC50 =0.1 and 0.5 µg/mL, respectively). FLZ-NP-PEI showed fungicidal activity even against C. glabrata and C. krusei (MFC =4 and 8 µg/mL, respectively). MIC50 values showed best results for FLZ-NPs and FLZ-NP-PEI. Nevertheless, only FLZ-NP-PEI displayed fungicidal activity against the studied strains. Keywords: drug delivery systems, double emulsion diffusion, nanoparticles, minimal inhibitory concentration, minimal fungicide concentration, polyethylenimineGómez-Sequeda NTorres ROrtiz CDove Medical PressarticleDrug delivery systemsDouble emulsion diffusion (DES-D)Nanoparticlesminimal inhibitory concentrationMICminimal fungicide concentrationMBCpolyethylenimine (PEI)Medical technologyR855-855.5Chemical technologyTP1-1185ENNanotechnology, Science and Applications, Vol Volume 10, Pp 95-104 (2017)
institution DOAJ
collection DOAJ
language EN
topic Drug delivery systems
Double emulsion diffusion (DES-D)
Nanoparticles
minimal inhibitory concentration
MIC
minimal fungicide concentration
MBC
polyethylenimine (PEI)
Medical technology
R855-855.5
Chemical technology
TP1-1185
spellingShingle Drug delivery systems
Double emulsion diffusion (DES-D)
Nanoparticles
minimal inhibitory concentration
MIC
minimal fungicide concentration
MBC
polyethylenimine (PEI)
Medical technology
R855-855.5
Chemical technology
TP1-1185
Gómez-Sequeda N
Torres R
Ortiz C
Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
description Nicolás Gómez-Sequeda,1 Rodrigo Torres,2 Claudia Ortiz3 1School of Biology, 2School of Chemistry, Faculty of Sciences, 3School of Microbiology, Faculty of Health, Universidad Industrial de Santander, Bucaramanga, Santander, Colombia Abstract: In this study, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) loaded with fluconazole (FLZ) and FLZ-NPs coated with the cationic polymer polyethylenimine (PEI) (FLZ-NP-PEI) were synthetized in order to improve antimycotic activity against four strains of Candida spp. of clinical relevance. FLZ-NPs and FLZ-NP-PEI were synthesized by double emulsion solvent-diffusion (DES-D) and characterized. Minimum inhibitory concentration (MIC50) and minimum fungicide concentration (MFC) were determined in vitro by culturing Candida strains in the presence of these nanocompounds. FLZ-NPs were spherical in shape with hydrodynamic sizes of ~222 nm and surface charge of -11.6 mV. The surface charges of these NPs were successfully modified using PEI (FLZ-NP-PEI) with mean hydrodynamic sizes of 281 nm and surface charge of 23.5 mV. The efficiency of encapsulation (~53%) and a quick release of FLZ (≥90% after 3 h) were obtained. Cytotoxicity assay showed a good cell viability for FLZ-NPs (≥86%), and PEI-modified NPs presented a decrease in cell viability (~38%). FLZ-NPs showed an increasing antifungal activity of FLZ for sensitive (Candida parapsilosis ATCC22019 and Candida albicans ATCC10231, MIC50 =0.5 and 0.1 µg/mL, respectively) and resistant strains (Candida glabrata EMLM14 and Candida krusei ATCC6258, MIC50 =0.1 and 0.5 µg/mL, respectively). FLZ-NP-PEI showed fungicidal activity even against C. glabrata and C. krusei (MFC =4 and 8 µg/mL, respectively). MIC50 values showed best results for FLZ-NPs and FLZ-NP-PEI. Nevertheless, only FLZ-NP-PEI displayed fungicidal activity against the studied strains. Keywords: drug delivery systems, double emulsion diffusion, nanoparticles, minimal inhibitory concentration, minimal fungicide concentration, polyethylenimine
format article
author Gómez-Sequeda N
Torres R
Ortiz C
author_facet Gómez-Sequeda N
Torres R
Ortiz C
author_sort Gómez-Sequeda N
title Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
title_short Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
title_full Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
title_fullStr Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
title_full_unstemmed Synthesis, characterization, and in vitro activity against Candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
title_sort synthesis, characterization, and in vitro activity against candida spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/8b23f649301a4073a2004c8cdbab9a16
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