Technology

Worldwide first water-free technology for ophthalmology

Novaliq F6H8 molekule

Topical eye drops are the mainstay of therapy for many ocular diseases, but features of existing water-based formulations create issues that can limit product efficacy and safety. Traditional aqueous vehicles for topical ophthalmic medications suffer from a number of limitations:

With water-based ophthalmic preparations, the typical dispensed drop size is 40 to 50 µL. This large volume exceeds the external eye’s reservoir capacity, resulting in spillover. The high surface tension of the aqueous-based drop further hinders 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. Together these factors reduce the residence time and contribute to the low bioavailability of conventional topical ophthalmic medications, which is reported to be as low as 3% to 4%.

Another limitation of using aqueous vehicles as a topical drug delivery platform relates to the fact that up to 60% of today’s new chemical entities are lipophilic compounds or large molecules that have poor water solubility.1 The addition of oils and/or surfactants into aqueous-based formulations offers a common strategy to address this problem, but the presence of these agents can lead to visual disturbance and tolerability issues. Tolerability can also be affected by preservatives that must be included in aqueous-based ophthalmic products that are packaged in conventional multi-dose containers.

EyeSol® is the first and only water-free technology for ocular drug delivery. It distinguishes from water-based technologies by a host of physical characteristics that translate into enhanced stability, bioavailability, efficacy, and tolerability.

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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

[1] @@fehlt

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