article · Journal of Pharmaceutical Innovation
Fluconazole nanoparticles coated with polyethylene glycol were developed and formulated into a Carbopol hydrogel to enhance topical delivery and antifungal performance. Using a solvent antisolvent precipitation method, nine formulations were tested to examine how polymer molecular weight and drug-to-polymer ratios affect particle size and entrapment efficiency. Polyethylene glycol molecular weight showed an antagonistic effect on particle size and an agonistic effect on entrapment efficiency. The resulting nanoparticles were uniform, spherical, and free from aggregations. When incorporated into Carbopol hydrogel, the optimised nanoparticles achieved greater drug release and significantly higher skin permeation compared to hydrogels carrying pure fluconazole. Drug release followed a first-order kinetic model and a super case II transport mechanism. Furthermore, agar well-diffusion tests demonstrated that the nanoparticle-loaded hydrogel produced larger inhibition zones, confirming improved antifungal activity over pure fluconazole.
Treating fungal infections effectively depends on ensuring sufficient amounts of medication can penetrate the skin. Fluconazole is widely used, but formulation barriers can limit its topical effectiveness. By incorporating polyethylene glycol-coated nanoparticles into a hydrogel, this technique improves drug release, skin permeation, and antifungal performance, providing a viable strategy to enhance existing antifungal treatments.
This work represents early-stage formulation research applicable to pharmaceutical companies developing improved topical antifungal products. The approach could enable manufacturers to enhance the delivery and skin absorption of poorly soluble active ingredients. However, the findings are based entirely on laboratory in vitro release, skin permeation, and agar-diffusion testing, meaning extensive preclinical safety evaluation and clinical trials are required before commercial use.
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The aim of this study was to prepare fluconazole (FLC) nanoparticles coated with polyethylene glycol (PEG) in the form of FLC-PEG-NPs and optimize the size and entrapment efficiency. Nine formulae were prepared by solvent antisolvent precipitation technique according to full 32 factorial designs. The effects of PEG molecular weight (X1) and the drug polymer ratio (X2) on the particle size (Y1) and entrapment efficiency (Y2) were explored. The prepared FLC-PEG-NPs were investigated for particle size, count rate, PDI, zeta potential, and morphology. Carbopol hydrogel was prepared, loaded with optimized FLC-PEG-NPs, and characterized for pH, FLC content, viscosity, homogeneity and spreadability, in vitro release, skin permeation, and antifungal activity. The formulated nanoparticles were uniform in size and spherical in shape with slightly rough surface and free from aggregations. The effect of PEG molecular was antagonistic on the particle size and was agonistic on EE %. The release of drug from hydrogel containing pure FLC was always lower than that from hydrogel containing FLC-PEG-NPs. The kinetic analysis of drug release obeys first-order release model and super case II transport mechanism. The cumulative amount of drug permeated applying hydrogel containing optimized FLC-PEG-NPs was significantly higher than the amount permeated using pure fluconazole containing hydrogel. The antifungal activity of hydrogel containing FLC in the form of optimized PEG-coated nanoparticles was better than hydrogel containing pure drug as indicated by relatively high inhibition zone using agar well-diffusion method. Small spherical FLC nanoparticles with enhanced in vitro drug release as well as improved antifungal activity could be achieved by using PEG-coated fluconazole nanoparticles.
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DOI: 10.1007/s12247-018-9335-z
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