Semifluorinated alkane technology brings advantages for topical therapy

November 1, 2016

Semifluorinated alkane technology has novel physicochemical properties that explain its benefits as an ocular lubricant and support its use for developing a well-tolerated, preservative-free, multidose preparation of cyclosporine.

Reviewed by Edward J. Holland, MD

Cincinnati, OH-Water-free vehicles based on semifluorinated alkane technology (EyeSol Platform Technology, Novaliq) have proven performance as an effective ocular lubricant and show promise for their ability to increase the solubility, stability, and bioavailability of topically delivered cyclosporine, said Edward J. Holland, MD.

The ocular lubricant contains perfluorohexyloctane (F6H8) and is already commercially available in Europe as an over-the-counter product (EvoTears).

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Currently, a phase II study is under way in the United States evaluating an investigational cyclosporine product (CyclASol, Novaliq) that formulates the immunomodulatory drug in the EyeSol Technology.

“Topical administration remains the mainstay for treatment delivery in ophthalmology, but local side effects can affect treatment adherence, and that is particularly true with cyclosporine,” said Dr. Holland, director of cornea services, Cincinnati Eye Institute, Cincinnati, OH. “The EyeSol vehicle allows for a preservative-free, multidose preparation of cyclosporine, and importantly, it may improve its tolerability.”

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Formulations based on the EyeSol Technology are clear, have a refractive index that is similar to water, and do not cause blurring of vision.

Moreover, they do not require preservatives because they do not support microbial growth, and because they do not contain water, they eliminate the potential for hydrolytic reactions that cause drug degradation, said Michael O’Rourke, president, Scotia Vision Life Science Consultants, Tampa, FL.

Clinical research

 

“The ocular lubricant supports the lipid layer of the tear film, but unlike lipid-based artificial tears, it does not cause blurring of vision,” he noted.

The EyeSol vehicle also has unique physical characteristics.

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“EyeSol has low viscosity and surface tension, and those characteristics result in a dispensed drop size that is about four times smaller than aqueous-based formulations,” O’Rourke explained.

“EyeSol formulations spread rapidly over the ocular surface without blinking,” he said. “This behavior minimizes any spillover and therefore enables increased drug delivery. In fact, results of ex vivo eye studies show that concentrations of cyclosporine achieved in ocular tissues were up to 10-fold greater using cyclosporine 0.05% in EyeSol compared with the commercially available 0.05% emulsion (Restasis, Allergan).”

Clinical research

The phase II study of cyclosporine formulated in EyeSol is a large, dose-finding, double-blind, multicenter investigation enrolling patients with moderate-to-severe dry eye. They were randomly assigned into one of four arms to receive twice daily treatment for four months with cyclosporine 0.1% in EyeSol, cyclosporine 0.05% in EyeSol, EyeSol vehicle, or the commercially available cyclosporine 0.05% ophthalmic emulsion.

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Results of a published study investigating the F6H8 ocular lubricant in patients with evaporative dry eye disease showed benefits after 6 weeks of four times daily treatment [Steven P, et al. J Ocul Pharmacol Ther. 2015;31:498-503].

Analyses of data from 25 of the 30 enrolled patients who completed the study per protocol showed significant improvements in corneal staining, Schirmer I score, and tear film break-up time, and symptoms assessed with the Ocular Surface Disease Index.

Dr. Holland noted that he has heard excellent feedback from European colleagues about the commercially available EvoTears ocular lubricant, particularly with respect to the comfort it provides.

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“The ability to improve patient comfort is critical for any dry eye treatment modality because bothersome symptoms are usually what brings patients to an eye care provider,” he said.

Pipeline portfolio

Novaliq is also leveraging its EyeSol platform for development of a topical omega-3 fatty acid preparation and for the treatment of glaucoma and retinal diseases.

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Edward J. Holland, MD

E: eholland@holprovision.com

Dr. Holland has been a consultant for Novaliq and is a consultant for other companies that market products for dry eye disease.