The Challenge with Conventional Eye Drops
Treating “front of the eye” diseases such as dry eye disease (DED), ocular graft versus host disease (oGVHD), glaucoma, allergic conjunctivitis, anterior uveitis and cataracts typically involves the use of topical eye drops. Conventional eye drops contain therapeutic drugs formulated in a liquid ophthalmic suspension. However, more than 90% of the drug contained in a conventional drop is lost into systemic circulation, leaving only a fraction of the total dose to reach target tissues and produce a therapeutic effect.
Ocugen developed its OcuNanoE™ technology platform to potentially enhance the effectiveness of its proprietary front of the eye therapeutics. Our OcuNanoE™ technology involves a proprietary process for formulating drug candidates into a unique ophthalmic nanoemulsion. Ocugen’s therapies are expected to have increased tear film stability, meaning a decreased drainage rate and prolonged residence time on the surface of the eye. This may enable better efficacy by allowing more of the active drug to reach the underlying ocular tissue. Ocugen plans to use its OcuNanoE™ formulation as a drug delivery system for the treatment of several ocular diseases, including its two lead Phase 3 drug candidates OCU300 and OCU310.
Ocugen believes its OcuNanoE™ formulation has several unique properties and benefits:
- Lipid components – act as the lipid layer of the tear film, both in functional characteristics and charge distribution;
- Optimal charge characteristics – allows drug molecules to reach the site of action without binding to the mucin layer;
- Optimal size – nanoemulsion enables drug molecules to transport through the interstitial cells to reach the specific target tissues;
- Preservative-free – reproducible nano size enables sterile filtration thus eliminating the need for preservatives, which can cause irritation
- Versatile and scalable – able to formulate both hydrophilic and lipophilic molecules at commercial scale
OcuNanoE™ – Enhanced Efficacy and Tissue Penetration
In preclinical studies of one of Ocugen’s lead candidates OCU300 (OcuNanoE™ brimonidine tartrate, 0.18%), OcuNanoE™ technology successfully improved overall efficacy, showing superiority to Restasis® (cyclosporine), lifitegrast (Xiidra®) and a marketed 0.2% brimonidine ophthalmic solution (approved for treating glaucoma).
Even at a 10% reduced dose compared to the current brimonidine ophthalmic solution, Brimonidine OcuNanoE™ achieved a reduction in ocular surface inflammation that was statistically significant (p<0.01) compared to the marketed brimonidine product. OCU300 also showed a positive trend with respect to reducing goblet cell loss while the 0.2% brimonidine tartrate ophthalmic solution did not differ from control groups.
In addition, Brimonidine (0.18%) OcuNanoE™ demonstrated enhanced preferential distribution of brimonidine to target tissues, such as lacrimal gland, where it exerts its biological function for treating ocular graft versus host disease (oGVHD) and dry eye disease. Achieving a therapeutic drug level in the lacrimal gland and other ocular tissues is a particular challenge for conventional eye drops, requiring increased dose of drug. In a preclinical animal model, brimonidine distribution in the lacrimal glands was approximately two-fold higher following a single dose of OcuNanoE™ compared to brimonidine ophthalmic solution (up to six hours).