Abstract
PurposeThe 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.MethodsNine 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.ResultsThe 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.ConclusionSmall spherical FLC nanoparticles with enhanced in vitro drug release as well as improved antifungal activity could be achieved by using PEG-coated fluconazole nanoparticles.
Highlights
Solubility enhancement of poor water-soluble drug is an important factor in preparing effective dosage form that can be either administered systemically or applied locally
FLC-polyethylene glycol (PEG)-NPs were obtained after evaporation of methanol
The solution was gradually changed from clear solution to cloudy indicating the formation of highly dispersed FLC-PEG-NPs
Summary
Solubility enhancement of poor water-soluble drug is an important factor in preparing effective dosage form that can be either administered systemically or applied locally. The size and morphology of the drug affect the biopharmaceutical properties such as solubility, dissolution rate, and absorption rates. Inclusion complexation, nanoparticles, and nanosuspension are the most extensively applied methods for improving drug solubility, stability, and bioavailability of active ingredients. The increased drug solubility by nanoparticles is attributed to the decreased particle size with subsequent increase in the surface area. Nanonization is the preparation of ultrafine nanoparticles by solvent evaporation. Nanonization is a simple, rapid, and low-cost method for enhancing the solubility and dissolution rate of poorly soluble drugs [3]. Nanoprecipitation is an alternative method that is widely applied for nanoparticle
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