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Published on: January 13, 2023
Biodegradable Polymers-based Nanoparticles to Enhance the Antifungal Efficacy of Fluconazole against Candida albicans
Noha Saleh1, Soha Elshaer2, Germeen Girgis1
1Pharmaceutics Department, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Background:
Fluconazole (FLZ), a potent antifungal medication, is characterized by poor water solubility that reduced its antifungal efficacy.
Objective:
This study aimed to prepare FLZ-loaded polymeric nanoparticles (NPs) by using different polymers and techniques as a method of enhancing the antifungal activity of FLZ.
Methods:
NP1, NP2, and NP3 were prepared by the double emulsion/solvent evaporation method using PLGA, PCL, and PLA, respectively. The ionotropic pre-gelation technique was applied to prepare an alginate/chitosan-based formulation (NP4). Particle size, zeta potential, encapsulation efficiency, and loading capacity were characterized. FT-IR spectra of FLZ, the polymers, and the prepared NPs were estimated. NP4 was selected for further in-vitro release evaluation. The broth dilution method was used to assess the antifungal activity of NP4 using a resistant clinical isolate of Candida albicans.
Results:
The double emulsion method produced smaller-sized particles (<390 nm) but with much lower encapsulation efficiency (<12%). Alternatively, the ionic gelation method resulted in nanosized particles with a markedly higher encapsulation efficiency of about 40%. The FT-IR spectroscopy confirmed the loading of the FLZ molecules in the polymeric network of the prepared NPs. The release profile of NP4 showed a burst initial release followed by a controlled pattern up to 24 hours with a higher percent released relative to the free FLZ suspension. NP4 was able to reduce the value of MIC of FLZ by 20 times.
Conclusion:
The antifungal activity of FLZ against C. albicans was enhanced markedly via its loading in the alginate/chitosan-based polymeric matrix of NP4.
Insights
This study developed fluconazole-loaded nanoparticles using alginate/chitosan, significantly enhancing antifungal efficacy against Candida albicans. The novel formulation improved drug delivery and potency.
Area of Science:
- Pharmaceutical Nanotechnology
- Antimicrobial Drug Delivery
Background:
- Fluconazole (FLZ) exhibits poor water solubility, limiting its antifungal effectiveness.
- Developing advanced drug delivery systems is crucial for improving FLZ's therapeutic potential.
Purpose of the Study:
- To formulate fluconazole-loaded polymeric nanoparticles (NPs) using various polymers and techniques.
- To enhance the antifungal activity of fluconazole through nanoparticle encapsulation.
Main Methods:
- Polymeric nanoparticles (NP1-NP3) were prepared using PLGA, PCL, and PLA via double emulsion/solvent evaporation.
- An alginate/chitosan-based formulation (NP4) was developed using ionotropic pre-gelation.
- Characterization included particle size, zeta potential, encapsulation efficiency, and FT-IR spectroscopy.
- In-vitro release and antifungal activity against Candida albicans were assessed for NP4.
Main Results:
- The ionotropic gelation method yielded nanosized particles (NP4) with high encapsulation efficiency (~40%), outperforming the double emulsion method (<12%).
- FT-IR confirmed successful encapsulation of fluconazole within the polymeric matrix.
- NP4 demonstrated a controlled release profile and a 20-fold reduction in the minimum inhibitory concentration (MIC) of fluconazole.
Conclusions:
- Alginate/chitosan-based nanoparticles (NP4) effectively enhance the antifungal activity of fluconazole.
- Nanoparticle formulation represents a promising strategy to overcome fluconazole's solubility limitations and improve efficacy against Candida albicans.
