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Enhanced antifungal efficacy of tebuconazole using gated pH-driven mesoporous nanoparticles.

Mas N, Galiana I, Hurtado S, Mondragón L, Bernardos A, Sancenón F, Marcos MD, Amorós P, Abril-Utrillas N, Martínez-Máñez R, Murguía JR - Int J Nanomedicine (2014)

Bottom Line: pH-sensitive gated mesoporous silica nanoparticles have been synthesized.Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole.Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Centro de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Centro Mixto Universidad Politécnica de Valencia, Universidad de Valencia, Valencia, Spain ; Departamento de Química, Universidad Politécnica de Valencia, Valencia, Spain ; CIBER de Bioingeniería, Biomateriales y Nanomedicina, Madrid, Spain.

ABSTRACT
pH-sensitive gated mesoporous silica nanoparticles have been synthesized. Increased extracellular pH and internalization into living yeast cells triggered molecular gate aperture and cargo release. Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole. Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity. As alterations of acidic external pH are a key parameter in the onset of fungal vaginitis, this nanodevice could improve the treatment for vaginal mycoses.

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Related in: MedlinePlus

Cell viability assay results of free tebuconazole and S1-Teb in the presence of Saccharomyces cerevisiae. Percentage colony formation unit (CFU) growth versus tebuconazole concentration in μg/mL is represented.Abbreviation: S1-Teb, MCM-41 loaded with tebuconazole.
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f4-ijn-9-2597: Cell viability assay results of free tebuconazole and S1-Teb in the presence of Saccharomyces cerevisiae. Percentage colony formation unit (CFU) growth versus tebuconazole concentration in μg/mL is represented.Abbreviation: S1-Teb, MCM-41 loaded with tebuconazole.

Mentions: Different solutions of free tebuconazole and suspensions of solid S1-Teb with several concentrations (0–200 μg tebuconazole/mL) were prepared by adding dimethyl sulfoxide 2× and SVF at a final volume of 200 μL and 2% dimethyl sulfoxide concentration. The amount of free drug used in the study was the same as that contained in the capped solid S1-Teb, calculated by elemental analysis and thermogravimetry studies (see Supplementary materials). Then, 100 μL of the aforementioned solutions or solid suspensions were added to the different Eppendorf vials containing 100 μL of the yeast suspension (for yeast preparation treatment see Supplementary materials). These final yeast suspensions containing different amounts of free tebuconazole or S1-Teb (0–100 μg tebuconazole/mL) were incubated for 6 hours at 37°C with no stirring. After the incubation period, approximately 300 cells were seeded in a YPD plate and incubated at 28°C for 72 hours. Finally, colony formation units (CFUs) were quantified. The results of the experiments containing duplicates were repeated twice (see Figure 4).


Enhanced antifungal efficacy of tebuconazole using gated pH-driven mesoporous nanoparticles.

Mas N, Galiana I, Hurtado S, Mondragón L, Bernardos A, Sancenón F, Marcos MD, Amorós P, Abril-Utrillas N, Martínez-Máñez R, Murguía JR - Int J Nanomedicine (2014)

Cell viability assay results of free tebuconazole and S1-Teb in the presence of Saccharomyces cerevisiae. Percentage colony formation unit (CFU) growth versus tebuconazole concentration in μg/mL is represented.Abbreviation: S1-Teb, MCM-41 loaded with tebuconazole.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4043724&req=5

f4-ijn-9-2597: Cell viability assay results of free tebuconazole and S1-Teb in the presence of Saccharomyces cerevisiae. Percentage colony formation unit (CFU) growth versus tebuconazole concentration in μg/mL is represented.Abbreviation: S1-Teb, MCM-41 loaded with tebuconazole.
Mentions: Different solutions of free tebuconazole and suspensions of solid S1-Teb with several concentrations (0–200 μg tebuconazole/mL) were prepared by adding dimethyl sulfoxide 2× and SVF at a final volume of 200 μL and 2% dimethyl sulfoxide concentration. The amount of free drug used in the study was the same as that contained in the capped solid S1-Teb, calculated by elemental analysis and thermogravimetry studies (see Supplementary materials). Then, 100 μL of the aforementioned solutions or solid suspensions were added to the different Eppendorf vials containing 100 μL of the yeast suspension (for yeast preparation treatment see Supplementary materials). These final yeast suspensions containing different amounts of free tebuconazole or S1-Teb (0–100 μg tebuconazole/mL) were incubated for 6 hours at 37°C with no stirring. After the incubation period, approximately 300 cells were seeded in a YPD plate and incubated at 28°C for 72 hours. Finally, colony formation units (CFUs) were quantified. The results of the experiments containing duplicates were repeated twice (see Figure 4).

Bottom Line: pH-sensitive gated mesoporous silica nanoparticles have been synthesized.Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole.Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Centro de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Centro Mixto Universidad Politécnica de Valencia, Universidad de Valencia, Valencia, Spain ; Departamento de Química, Universidad Politécnica de Valencia, Valencia, Spain ; CIBER de Bioingeniería, Biomateriales y Nanomedicina, Madrid, Spain.

ABSTRACT
pH-sensitive gated mesoporous silica nanoparticles have been synthesized. Increased extracellular pH and internalization into living yeast cells triggered molecular gate aperture and cargo release. Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole. Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity. As alterations of acidic external pH are a key parameter in the onset of fungal vaginitis, this nanodevice could improve the treatment for vaginal mycoses.

Show MeSH
Related in: MedlinePlus