Clathrated Antioxidant Ophthalmic Composition for Dry Eye
Solution Overview
Problem
Current ophthalmic therapies lack effective solutions for increasing tear volume and goblet cell count, which are crucial for treating and preventing conditions like dry eye and other ophthalmic diseases, as existing antioxidants are poorly soluble in aqueous solutions, limiting their efficacy.
Innovation Solution
A clathrated ophthalmic composition comprising a lipid-soluble antioxidant, such as astaxanthin, combined with a macrocyclic compound like cyclodextrin, which enhances water solubility and bioavailability, allowing for increased tear volume and goblet cell count, thereby addressing dry eye and other ophthalmic issues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If lipid-soluble antioxidants are used in ophthalmic compositions, then antioxidant efficacy is improved, but water solubility deteriorates
Solution Approach 1:
The patent employs cyclodextrin as a host compound that forms an inclusion complex with the lipid-soluble antioxidant. The cyclodextrin acts as an intermediary that solubilizes the hydrophobic antioxidant in aqueous ophthalmic solutions, enabling both water solubility and antioxidant efficacy to coexist. The host-guest inclusion complex allows the antioxidant to be delivered effectively in tear-drop formulations.
2Quantity of substance
If antioxidants are administered orally as nutritional supplements, then antioxidant intake is improved, but targeted delivery to ocular surface deteriorates
Solution Approach 1:
The patent extracts the antioxidant benefit from systemic oral administration and delivers it directly to the ocular surface through topical application. By formulating the antioxidant in an ophthalmic composition that can be administered as eye drops, the invention achieves localized high concentration at the target site (ocular surface) while maintaining antioxidant efficacy, thereby improving targeted delivery compared to oral supplementation.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The clathrated antioxidant composition significantly improves tear volume and goblet cell count, effectively treating and preventing dry eye and similar ophthalmic diseases by improving the solubility and bioavailability of lipid-soluble antioxidants in aqueous solutions.
Implementation Method 1
A clathrated ophthalmic composition comprising a lipid-soluble antioxidant, such as astaxanthin, combined with a macrocyclic compound like cyclodextrin, which enhances water solubility and bioavailability
Data Source
AI summary
The present invention provides an ophthalmic composition and a use thereof. In one embodiment of the present invention, an ophthalmic composition containing a clathrated antioxidant substance is provided. In some of embodiments of the present invention, a composition for treating or preventing an ophthalmic disease, an ophthalmic disorder or an ophthalmic symptom is provided, wherein the ophthalmic disease, the ophthalmic disorder or the ophthalmic symptom includes, but is not limited to, dry eye or a dry eye-like ophthalmic disease, conjunctivitis, corneal ulcer, age-related macular degeneration, cataract, pseudoexfoliation syndrome, and symptoms in these diseases which can be ameliorated by increasing the quantity of tears and/or goblet cells and/or mucin.