Choline Ester of Lipoic Acid for Ocular Oxidative Damage

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Solution Overview

Problem

Age-related conditions such as presbyopia and cataract pose challenges due to decreased accommodative amplitude and oxidative stress, with existing treatments often causing toxicity to surrounding healthy tissues.

Innovation Solution

The use of the choline ester of lipoic acid as a reducing agent, administered topically for ocular delivery, which reduces disulfide bond formation and oxidative damage in lens cells, potentially treating or preventing presbyopia and cataract while minimizing toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for presbyopia and cataract are used, then vision correction is achieved, but toxicity to surrounding healthy tissues occurs

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtoxicity to healthy tissues

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameter by using choline ester of lipoic acid instead of conventional reducing agents. This parameter change maintains treatment effectiveness while reducing toxicity to healthy tissues through the unique properties of the choline ester formulation

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The choline ester of lipoic acid acts as an intermediary substance that delivers the therapeutic effect of lipoic acid while the choline component reduces direct toxicity to surrounding healthy tissues. The intermediary formulation allows controlled delivery and reduced harmful effects

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of moving object

If reducing agents are used to treat lens stiffness, then accommodative amplitude increases, but oxidative stress in surrounding tissues may increase

Engineering Contradiction:

Improveaccommodative amplitudeVSAvoidoxidative stress

Core Design Contradiction:

Duration of action of moving objectVSObject-generated harmful factors

Solution Approach 1:

The patent converts the potential harmful oxidative stress into a beneficial effect by using lipoic acid, which is a potent antioxidant. The choline ester formulation enhances this benefit by reducing lens stiffness through disulfide bond reduction while simultaneously protecting surrounding tissues from oxidative damage

Inventive Principle:

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

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 choline ester of lipoic acid effectively reduces lens stiffness and oxidative damage, maintaining or increasing accommodative amplitude and reducing lens opacity, thereby addressing age-related vision issues effectively and safely.

Implementation Method 1

The use of the choline ester of lipoic acid as a reducing agent, administered topically for ocular delivery, which reduces disulfide bond formation and oxidative damage in lens cells

Methodology Applied

Scientific EffectReduction: Reduction

Implementation Method 2

The choline ester of lipoic acid effectively reduces lens stiffness and oxidative damage

Methodology Applied

Scientific EffectOxidation: Oxidation

Data Source

PatentEP2821405B1Choline esters for treating presbyopia and cataract

Publication Date: 2016.04.13 ENCORE HEALTH LLC

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AI summary

Compounds having a formula selected from: or (R)-2-(dimethylamino)ethyl 5-(1,2-dithiolan-3-yl)pentanoate, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.