Transport of Vitamin E from Ethanol/Water Solution into Contact Lenses and Impact on Drug Transport

Purpose: Contact lens-based drug delivery has many advantages over eye drops including higher bioavailability and sustained release. Commercial contact lenses release drug rapidly necessitating integration of control-release mechanisms into the lenses such as incorporation of vitamin E diffusion barriers. In prior publications, vitamin E barriers are loaded by placing the lenses in vitamin E-ethanol solution, followed by the ethanol extraction. In this article, we investigate feasibility of manufacturing vitamin E barriers by soaking contact lenses in vitamin E dissolved in ethanol-water solutions to minimize swelling.Methods: Contact lenses are soaked in solutions of vitamin E dissolved in ethanol-water mixtures. The dynamics of vitamin E transport into the measured and fitted to diffusion equation to determine diffusivity and partition coefficient. Vitamin E loaded lenses are imaged and transport of hydrophilic drug timolol is measured.Results: The partition coefficient of vitamin E increases more than 5 and 10-fold when the water content in the loading solution reaches 15% and 25% (v/v), respectively. The solubility of vitamin E in the solutions decreases as water fraction increases but the increase in partition coefficient allows for loading > 20% vitamin E in the lens. The barriers manufactured by this approach are effective at sustaining release of glaucoma drug timolol.Conclusions: Vitamin E barriers can be incorporated into contact lenses by soaking in solutions of vitamin E in water and ethanol. Vitamin E barriers extended hydrophilic drug release and the reduced swelling is beneficial in minimizing the possibility of lens damage during loading of vitamin E.

Automated summary

This study investigates the feasibility of manufacturing vitamin E diffusion barriers in contact lenses by soaking them in vitamin E dissolved in ethanol-water solutions to minimize swelling. The results showed that the partition coefficient of vitamin E increases significantly with higher water content in the loading solution, allowing for the loading of a higher percentage of vitamin E in the lens. The barriers manufactured by this approach effectively sustain the release of the glaucoma drug timolol.