Technology

Worldwide first and only water-free technology for ophthalmology

Novaliq F6H8 molekule

Topical eye drops are the therapeutic pillar for many ocular diseases, but traditional water-based formulations have significant limitations that may influence efficacy and safety.

Water-based ophthalmic preparations dispense a typical drop size of 40 to 50 µL. This volume exceeds the external eye’s reservoir capacity, causing spill-over from the eye. The surface tension of water further limits its spreading on the ocular surface. In addition, the application of an aqueous-based eye drop can activate the defense mechanism of the eye with rapid blinking after instillation and tear secretion. All these factors reduce the retention time and contribute to a relatively low bioavailability of traditional topical ophthalmic medications, which is reported to be between 1-10%.

Another limitation of using aqueous formulations relates to the fact that up to 60% of today’s new chemical entities are lipophilic compounds or large molecules with poor water solubility. The addition of mineral oils and/or surfactants into aqueous-based and/or blurred vision. Tolerability can also be affected by preservatives that are often required in multi-dose containers.

EyeSol® is the worldwide first and only water-free technology for ophthalmic products. It dramatically increases the residual time on the eye from minutes to hours and enables high bioavailability of active pharmaceutical ingredients (API) with excellent tolerability and safety while reducing systemic exposure due to a small drop size (10 µL).

EyeSol® unlocks the full potential of APIs by generating novel drug products often even with new Composition of Matter IP. The technology is clinically validated, safe and well accepted.

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What is special about EyeSol®?

EyeSol® is based on specific semifluorinated alkanes (SFAs). These compounds have the same refractive index as water and are transparent, inert, non-toxic, amphiphilic liquids that are able to formulate lipophilic and large molecules, such as biologic agents. Because they have very low surface tension and viscosity, SFAs dispense as a low volume drop (<12 µL) that does not stimulate blinking or reflex tearing. Having both low surface tension and low interface tension, EyeSol® products spread rapidly over the ocular surface and form a flat, transparent monolayer that enables clear vision without blurring. Because of their amphiphilic nature, EyeSol® products also interact with tear film lipids and have been shown to stabilize and restore the tear film.

Being aqueous-free, EyeSol® products avoid hydrolytic and oxidative reactions that can degrade active pharmaceutical ingredients, thus improving product stability. In addition, the aqueous-free EyeSol® technology platform does not support microbial growth, and therefore it allows manufacturing of preservative-free formulations in multi-dose containers. It also avoids problems of tip clogging that can occur with suspensions.


Sources

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