S.P. Barman, K. Barman, S. Harris, K. Ward
Symphony Therapeutics (subsidiary of Integral BioSystems),
United States
Keywords: lipid nanoparticles, anti-oxidant, UV-block
Summary:
UV exposure of ocular tissues has been linked to multiple disorders of the eye, some of which can lead to blindness. These disorders are corneal pterygium (ocular surface growths), corneal blebs, corneal and scleral burns, cataract formation, corneal thinning, corneal ulcers, retinal burns, glaucoma and macular degeneration. According to the World Health Organization (WHO), corneal blindness is the 4th largest cause of blindness worldwide where either loss of transparency or distortion of the refractive surface causes vision impairment [23]. Chronic exposure to UV can cause damage to the anterior pole of the eye, ranging from minor (pterygium) to serious photokeratitis. In the veterinary markets, UV damage to ocular tissues can lead to corneal opacity, pannus, cataracts and ocular carcinoma. UV radiation from sunlight is categorized based on wavelength: UVA (315-400 nm), UVB (280-315 nm) and UVC (100-280 nm). More than 90% of UVB and 60% of UVA radiation is absorbed by the cornea, whereas the retina and deeper ocular tissues absorbed UV light in the range 300-800 nm, with the most phototoxic effect on the retina at wavelengths around ~430 nm (“blue light”). UV light that damages ocular tissues are primarily due to UVA and UVB (UVC is filtered out by the ozone layer), causing photochemical damage to cellular DNA due to the spontaneous production of reactive oxygen species. The production of reactive oxygen species elicits the production of pro-inflammatory species causing degeneration of critical ocular tissues. There are no ophthalmic products with UV-blocking properties. We have developed OcuHeal-UV400+, a lipid nanoparticle eye-drop product that contains a plant-based flavonoid, found abundantly in fruit and vegetables. The molecule IB0801 is a small molecule of molecular weight < 500 Daltons, has FDA GRAS status as an oral supplement, has been shown to have anti-oxidant capabilities, is biocompatible to the ocular surface and blocks portions of UVA and UVB. When incorporated/encapsulated into Symphony’s proprietary lipid nanoparticle technology (OcuHeal™), UV light wavelengths from 200-550 nm are blocked. Additionally, it’s potent anti-oxidant and anti-inflammatory properties renders a healing and protective effect to the ocular surface. We present data that demonstrates the UV-blocking properties of the product, protective effect on corneal and retinal cells in the presence of UV light, downregulation of inflammatory markers and stability data. Manufacturing and sterilization processes have been worked out to enable a sterile, ophthalmic product. The utility of this product as a preventive and curative measure to UV damage on the ocular surface is extraordinary. Currently, there are no ophthalmic UV-protective medications in either the veterinary or human markets. The OcuHeal-UV400+ technology is based on a proprietary platform technology, that has been wholly patented in 12 global jurisdictions. The UV-protective technology can be also be extended into an eyelid wipe to block damaging UV radiation. Currently, there are no biocompatible UV products to protect sensitive “around-the-eye” area from UV damage.