Antioxidant Eye Drops for Cataract and Dry Eye Relief

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Solution Overview

Problem

Current treatments for age-related ocular diseases such as cataracts and macular degeneration are limited, with no established pharmaceutical treatments for cataracts and inadequate medical interventions for preventing or reducing dry eye conditions, which are exacerbated by oxidative stress and iron overload.

Innovation Solution

Topical antioxidant eye drops containing astaxanthin, resveratrol, ethyl pyruvate, and epigallocatechin gallate in a carbomer gel carrier, along with ethylenediaminetetraacetic acid (EDTA), which reduce oxidative stress through free radical scavenging and chelating activity, delaying cataract progression and reducing retinal degeneration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If oral administration of antioxidant formulations is used, then systemic antioxidant levels are improved, but ocular tissue concentration and direct protective effect are insufficient

Engineering Contradiction:
Improvesystemic antioxidant levelsVSAvoidocular tissue protection efficacy
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent uses a carbomer gel carrier as an intermediary delivery system that facilitates direct ocular administration of antioxidants. The gel matrix enables controlled release and sustained contact with ocular surfaces, bridging the gap between topical application and effective tissue delivery, thereby achieving reliable ocular protection without relying on systemic circulation

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention segments the antioxidant delivery system into four distinct active ingredients (astaxanthin, resveratrol, ethyl pyruvate, and epigallocatechin gallate), each with specific antioxidant and chelating properties. This segmentation allows for targeted protection against different oxidative mechanisms in ocular tissues while maintaining individual stability and efficacy

Inventive Principle:
Principle #1Segmentation

2Reliability

If cataract surgery is performed, then vision restoration is achieved, but incidence of late AMD increases

Engineering Contradiction:
Improvevision restorationVSAvoidlate AMD incidence
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary antioxidant protection to delay cataract formation and progression before surgical intervention becomes necessary. By establishing a baseline of oxidative stress protection through topical antioxidant application, the treatment aims to postpone the point at which surgical intervention is required, thereby potentially reducing exposure to surgical risks and associated complications

Inventive Principle:
Principle #10Preliminary action

3Use of energy by moving object

If oxidative stress is increased, then metabolic processes are enhanced, but tissue damage and disease progression occur

Engineering Contradiction:
Improvemetabolic activityVSAvoidoxidative damage
Core Design Contradiction:
Use of energy by moving objectVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful effects of oxidative stress into beneficial protective mechanisms by utilizing antioxidants that specifically target and neutralize reactive oxygen species. The four antioxidant ingredients work synergistically to scavenge free radicals and chelate iron, transforming the potentially damaging oxidative environment into a controlled state that maintains metabolic function while preventing tissue damage

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

4Use of energy by moving object

If iron levels are increased, then oxygen transport is improved, but hydroxyl radical formation and mitochondrial dysfunction increase

Engineering Contradiction:
Improveoxygen transport efficiencyVSAvoidhydroxyl radical generation
Core Design Contradiction:
Use of energy by moving objectVSObject-generated harmful factors

Solution Approach 1:

The patent introduces chelating agents as intermediary substances that bind to excess iron in ocular tissues, preventing direct interaction between iron and oxygen that would generate hydroxyl radicals. The carbomer gel carrier also serves as an intermediary delivery system that facilitates controlled release of chelating agents to maintain iron at protective rather than harmful levels

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3203993B1Antioxidant eye drops
Publication Date: 2021.07.21 KADOR PETER F
  • EP3203993B1 patent drawingFigure 1
  • EP3203993B1 patent drawingFigure 2
  • EP3203993B1 patent drawingFigure 3

AI summary

The antioxidant eye drops is a topical ophthalmic formulation that contains four nutraceuticals (namely, astaxanthin, resveratrol, pyruvate and epigallocatechin gallate (EGCG)) having antioxidant, anti-inflammatory, and chelating activity in a carbomer gel carrier. The active ingredients can reduce oxidative stress through free radical scavenging and chelating activity. The carrier is composed of a solution of deionized water containing about 0.4% Carbopol 980 NF, 5.7% sorbitol. 0.01% cetrimide, 0.01% EDTA, and sodium chloride and sodium hydroxide in adequate amounts to adjust both the viscosity and the pH of the topical carrier to pH 7.0-7.4. Use of the formulation may delay the development of cataracts, reduce retinal degeneration, and maintain normal tear flow in dry eye due to the antioxidant, anti-inflammatory, and chelating activity of the active ingredients.