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Pluronic F-127 Enhances the Antifungal Activity of Fluconazole against Resistant Candida Strains

Candida strains as the most frequent causes of infections, along with their increased drug resistance, pose significant clinical and financial challenges to the healthcare system. Some polymeric excipients were reported to interfere with the multidrug resistance mechanism. Bearing in mind that there are a limited number of marketed products with fluconazole (FLU) for the topical route of administration, Pluronic F-127 (PLX)/FLU formulations were investigated in this work. The aims of this study were to investigate (i) whether PLX-based formulations can increase the susceptibility of resistant Candida strains to FLU, (ii) whether there is a correlation between block polymer concentration and the antifungal efficacy of the FLU-loaded PLX formulations, and (iii) what the potential mode of action of PLX assisting FLU is. The yeast growth inhibition upon incubation with PLX formulations loaded with FLU was statistically significant. The highest efficacy of the azole agent was observed in the presence of 5.0 and 10.0% w/v of PLX. The upregulation of the CDR1/CDR2 genes was detected in the investigated Candida strains, indicating that the efflux of the drug from the fungal cell was the main mechanism of the resistance.

 

Comments:

It seems like you're discussing a study that explores the potential of Pluronic F-127 (PLX)/fluconazole formulations in addressing drug-resistant Candida strains. The research investigates whether these formulations could enhance susceptibility, the correlation between polymer concentration and antifungal efficacy, and the potential mode of action of PLX in assisting fluconazole.

The study's findings indicate that the PLX formulations loaded with fluconazole led to statistically significant inhibition of yeast growth. Notably, the highest efficacy of the antifungal agent was observed when using 5.0% and 10.0% w/v concentrations of PLX. Additionally, the investigation detected upregulation of the CDR1/CDR2 genes in the studied Candida strains, suggesting that drug efflux from the fungal cell was the primary mechanism of resistance.

This research could be crucial in addressing the challenges posed by drug-resistant Candida strains, especially considering the limited number of available products with fluconazole for topical administration. The findings suggest that PLX-based formulations might offer a promising avenue for enhancing the effectiveness of fluconazole against these resistant strains.

Related Products

Cat.No. Product Name Information
S6936 Pluronic F-68 Pluronic F-68 (Poloxamer 188, P188, MST-188) is a triblock copolymer of the form polyethylene oxide-polypropylene oxide-polyethylene oxide (PEO-PPO-PEO) with surface-active properties. Pluronic F-68 is used in the pharmaceutical industry as an excipient in various formulations and drug delivery systems. Pluronic F-68 is effective in the repair/recovery of damaged cell membranes.

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