Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity
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Date
2019
Journal Title
Journal ISSN
Volume Title
Type
Article
Publisher
Springer New York LLC
Series Info
Journal of Pharmaceutical Innovation
14
14
Scientific Journal Rankings
Abstract
Purpose: 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. Methods: 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. Results: 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. Conclusion: 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. 2018, The Author(s).
Description
Scopus
Keywords
Fluconazole, Nanoparticles, Polyethylene glycol, Skin permeation, carbopol 940, fluconazole, macrogol, polymer, animal experiment, antifungal activity, Article, clinical effectiveness, controlled study, dispersity, drug release, drug solubility, factorial design, hydrogel, in vitro study, material coating, molecular biology, molecular weight, nonhuman, particle size, PEGylation, precipitation, priority journal, rat, viscosity, zeta potential, zone of inhibition