The Problem: UV Exposure and Ocular Tissue Damage

Ultraviolet radiation is absorbed by multiple structures of the eye and is correlated with a range of ocular disorders, including corneal pterygia, cataracts, keratoconus, glaucoma, choroidal neovascularization (CNV), and age-related macular degeneration (AMD). UVR is categorized into three bands: UVA (315–400 nm), UVB (280–315 nm), and UVC (100–280 nm).

The cornea absorbs more than 90% of UVB and approximately 60% of UVA, while the retina absorbs UVA and blue light in the 300–800 nm range. At the cellular level, UVA and UVB cause damage to DNA through the production of reactive oxygen species (ROS), which trigger tissue-damaging inflammatory cytokines. The cumulative effect of this oxidative stress contributes to the progression of multiple ocular conditions over time.

Despite the well-established link between UV exposure and ocular disease, there is no widely adopted topical ophthalmic product that combines UV-blocking properties with antioxidant and anti-inflammatory activity in a single formulation designed for sustained ocular surface residence.

OcuHeal-UV400+: A Lipid Nanoparticle Eye Drop with UV-Blocking and Antioxidant Properties

Integral BioSystems developed OcuHeal-UV400+, a lipid nanoparticulate (LNP) eye drop formulated using its proprietary OcuHeal LNP technology platform. The product contains IB0108, a GRAS-designated antioxidant compound with decades of safe use as an oral supplement in humans and animals.

Key attributes of IB0108 and the OcuHeal-UV400+ formulation include:

• IB0108 is an FDA GRAS compound approved for daily oral consumption as a dietary supplement.
• It functions as an ROS quencher and antioxidant with anti-inflammatory, immunoprotective, and UV-protective properties.
• IB0108 blocks portions of UVA and UVB radiation in a dose-responsive manner.
• When encapsulated in the OcuHeal™ LNP platform, the entire UV wavelength range from 200 to 600 nm is blocked, extending coverage across UVA, UVB, and UVC.
• The OcuHeal™ LNP platform uses lipid nanocores with a particle size under 200 nm, enabling penetration of the ocular mucosal meshwork pores (approximately 500 nm).
• OcuHeal™ patents have been granted in 14 global jurisdictions.

A stabilized form of IB0108 was also developed, enabling short-term storage at 25°C/60% relative humidity. Stability recovery data showed greater than 88% recovery at 1 week and greater than 92% recovery at 12 weeks for the stabilized formulation, compared to lower recovery rates for the original form of the molecule.

Research Design and Methods

The research, presented at the 2025 ARVO Annual Meeting (Poster 4341 – A0497), characterized OcuHeal-UV400+ across UV-blocking efficacy, corneal cell protection, pharmacokinetic distribution in ocular tissues, and in vivo safety and tolerability.

OcuHeal-UV400+ was prepared as a nano-dispersion using a proprietary process. IB0108 content was measured by HPLC (Shimadzu Prominence). Particle size distribution was determined by laser diffraction (Horiba 950V2). UV-blocking properties were measured by UV-Vis spectrometry (Shimadzu). IB0108 incubation studies with human corneal epithelial cells (HCEC) in the presence of UVB (254 nm) were performed at the University of Waterloo. Bioanalytical analysis of ocular tissues was performed by LC/MS/MS using a validated method across cornea, iris/ciliary body, lens, retina, optic nerve, conjunctiva, sclera, eyelids, tear fluid, aqueous humor, and vitreous humor. Blood was analyzed for systemic exposure. Safety and tolerability were assessed in New Zealand White Rabbits using the SPOTS scoring system (Eaton et al. 2017) at 1, 2, 4, and 6 hours post-dosing.

Key Findings from the Research

The following results are relevant for teams evaluating ophthalmic formulation development strategies for UV-protective or antioxidant ophthalmic products:

UV-blocking efficacy:

IB0108 demonstrated dose-responsive UV-blocking behavior, with lower percent transmittance (higher UV blocking) at increasing concentrations. When encapsulated in the OcuHeal™ LNP, the formulation blocked the entire UV wavelength range from 200 to 600 nm, covering UVA, UVB, and UVC. This represents a significant enhancement over the UV-blocking characteristics of IB0108 alone.

Protection of human corneal epithelial cells:

In studies conducted at the University of Waterloo, IB0108 demonstrated a protective effect on human corneal epithelial cells (HCEC) exposed to UVB radiation at 254 nm. Cell viability data showed that IB0108 reduced UV-induced damage in a concentration-dependent manner, supporting the compound’s potential as a corneal cytoprotective agent.

Pharmacokinetic distribution across ocular tissues:

Following a single 80 mcg dose of IB0108 in OcuHeal eye drops administered to New Zealand White Rabbits, recovered concentrations of IB0108 were detected across multiple ocular tissues at 1, 2, 4, and 6 hours post-dosing. Tissues analyzed included the cornea, iris/ciliary body, lens, retina, optic nerve, and conjunctiva. Higher concentrations were observed in the conjunctiva, sclera, tear fluid, and eyelids, consistent with topical ocular delivery. The data demonstrate enhanced residence time on the ocular surface, with measurable IB0108 concentrations persisting through the 6-hour timepoint.

In vivo safety and tolerability:

OcuHeal-UV400+ lipid nanoparticles were assessed for signs of non-biocompatibility on the ocular surface at all timepoints, including IOP testing, redness, eyelid swelling, discharge, hyperemia, and corneal opacity, using the SPOTS scoring system. All scores were zero at all timepoints, indicating no adverse effects on any evaluated ocular parameter.

Formulation stability:

A novel stabilized form of IB0108 enabled short-term storage at 25°C/60% RH. The stabilized formulation maintained greater than 92% recovery at 12 weeks, compared to approximately 52.6% for the original form under the same conditions. This stability profile supports the feasibility of room-temperature storage and practical shelf-life requirements for a commercial ophthalmic product.

What This Means for Ophthalmic Development Teams

For R&D and product development teams working on UV-protective, antioxidant, or anti-inflammatory ophthalmic compounds, this research highlights several practical considerations:

• Encapsulation of a GRAS antioxidant in an LNP platform extended UV-blocking coverage from partial UVA/UVB to the full 200–600 nm range, covering UVA, UVB, and UVC.
• The OcuHeal™ LNP eye drop demonstrated a 6-hour ocular surface residence time with distribution across multiple ocular tissues, including posterior segment structures such as the retina and optic nerve.
• Zero adverse effects were observed across all SPOTS scoring parameters at all timepoints in preclinical testing.
• The stabilized formulation supports room-temperature storage, an important consideration for commercial viability and patient convenience.
• The product can function as a standalone UV-protective antioxidant eye drop or serve as a platform for formulating additional ophthalmic actives within the OcuHeal™ LNP system.

Integral BioSystems’ expertise in LNP-based ophthalmic delivery, combined with the OcuHeal™ platform, positions the company to support drug development services for UV-protective, antioxidant, and anti-inflammatory ophthalmic programs from feasibility through process engineering.

Read the Full Research

This blog post summarizes key findings from the ARVO 2025 poster by Barman K, Harris, Coleman, Belen, Ward, and Barman SP (Poster 4341 – A0497). To review the complete research, including UV-Vis spectrometry data, HCEC protection results, pharmacokinetic tissue distribution, tolerability scores, and stability data, download the full poster (PDF).

Explore all Integral BioSystems research on the publications page.

Discuss Your Ophthalmic Development Program

Whether you are evaluating LNP-based delivery for an ophthalmic antioxidant, exploring UV-protective formulations, or considering the OcuHeal™ platform for your compound, Integral BioSystems can support your program from feasibility through process engineering. Request a formulation consult to discuss your molecule and delivery objectives.