Ocular Delivery of Quercetin Using Microemulsion System: Design, Characterization, and Ex-vivo Transcorneal Permeation.

BACKGROUND

The goal of this research was to design and characterize quercetin microemulsions (MEs) to resolve water solubility issues related to quercetin and improve transcorneal permeation into the eye.

METHODS

MEs were prepared by the phase diagram method. Oily phase (oleic acid-Transcutol P), surfactant (Tween 80, Span 20), and co-surfactant (propylene glycol) were used to make a quercetin-loaded ME. The size of the droplets, their viscosity, pH, release, flux, and diffusivity were all measured.

RESULTS

Droplet diameters in ME samples ranged from 5.31 to 26.07 nanometers. The pH varied from 5.22 to 6.20, and the release test revealed that 98.06 percent of the medication was released during the first 24 hours. The flux and diffusivity coefficients of the ME-QU-8 formulation were 58.8 µg/cm.h and 0.009 cm/h, respectively, which were 8.8 and 17.9 times greater than the quercetin aqueous control (0.2 percent). The maximum percentage of drug permeated through rabbit cornea after five hours was 16.11%.

CONCLUSIONS

It is concluded that ME containing quercetin could increase transcorneal permeation and that permeation could be altered by any change in the composition of the ME formulation. This effect might be caused by structural alterations in the cornea caused by ME components.