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

Abstract

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/cm2.h and 0.009 cm2/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.

Physicochemical Characterization, Release and Penetration Study of Nanostructured Lipid Carriers Quercetin Incorporated into Membrane-Type Patches

“…The use of stearic acid and oleic acid as a lipid matrix result in the high quercetin entrapment efficiency because both of these lipids can make quercetin more soluble, which increases the likelihood that it will be trapped in NLC particles. 24,25 3. The SEM image captures the surface of the membrane-type patch (Figure 2).…”

Development of rutin-loaded nanostructured lipid carriers for improved ocular delivery: Optimization, in vitro, ex vivo, and toxicity evaluation

“…Moreover, transcorneal permeability studies were also performed to determine the permeability coe cient, which was also considered in the optimization process. An in vitro release study was conducted to examine the release of rutin from its encapsulated form (RT-NLC) using the Franz diffusion cell method [23]. A barrier made of activated cellulose membrane-60 (LA390, HIMEDIA) was placed between the donor and receptor compartments of the Franz diffusion cell.…”

Preparation, Characterization, and Skin Permeation Evaluation of Naproxen Microemulsions for Transdermal Delivery

“…NPX-MEs were constructed following the same formulations used in our previous works (21). A full factorial design, as a convenient method to prepare MEs, was used with three variables at two levels.…”