Levodopa Ophthalmic Compositions for Intraocular Dopamine Elevation

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Solution Overview

Problem

Current treatments for visual disorders such as myopia, diabetic retinopathy, and Parkinson's disease associated with reduced dopamine levels in the eye are limited by adverse effects and lack of targeted intraocular dopamine elevation, and geographical and social barriers hinder outdoor exposure for myopia prevention.

Innovation Solution

Aqueous formulations of levodopa combined with an antioxidant penetrate ocular tissues to elevate intraocular dopamine levels, inhibiting the progression or development of visual disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If oral administration of levodopa is used to elevate dopamine levels, then dopamine levels in the central nervous system are elevated, but dopamine levels in the eye are not sufficiently elevated and systemic side effects occur

Engineering Contradiction:
Improvedopamine levels in the eyeVSAvoidsystemic side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The invention divides the treatment approach into localized ocular administration rather than systemic oral administration. The composition is applied topically to the eye, segmenting the therapeutic action to specifically target ocular tissues and elevate intraocular dopamine levels without significantly affecting systemic dopamine levels, thereby resolving the contradiction between achieving sufficient dopamine elevation in the eye and avoiding systemic side effects

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention applies levodopa locally to ocular tissues through topical administration. The aqueous composition is designed to penetrate ocular barriers and deliver levodopa specifically to the eye, creating a local high concentration of dopamine in ocular tissues while maintaining low systemic exposure, thus achieving the desired local effect without systemic harmful factors

Inventive Principle:
Principle #3Local quality

2Quantity of substance

If time spent outdoors in bright light is increased to prevent myopia, then dopamine levels in the eye are elevated, but geographical and social barriers prevent sufficient exposure

Engineering Contradiction:
Improvedopamine levels in the eyeVSAvoidflexibility of treatment application
Core Design Contradiction:
Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The invention uses levodopa as an intermediary substance that can be administered topically to the eye. Instead of relying on light exposure as the direct method to elevate dopamine levels, the composition serves as a mediator that delivers the necessary dopamine precursor directly to ocular tissues, bypassing the need for geographical and social conditions that enable outdoor exposure

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the approach from environmental parameter control (light exposure duration and intensity) to pharmacological parameter control (topical application of levodopa composition). This allows dopamine levels in the eye to be elevated through a controllable pharmaceutical parameter rather than being dependent on external environmental factors beyond the subject's control

Inventive Principle:
Principle #35Parameter changes

3Reliability

If atropine is used to reduce myopia progression, then the rate of myopia progression is reduced, but posttreatment rebound effects and significant adverse effects occur

Engineering Contradiction:
Improveeffectiveness in reducing myopia progressionVSAvoidposttreatment rebound effects and adverse effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention changes the pharmacological parameter from using atropine (a muscarinic antagonist) to using levodopa (a dopamine precursor). This parameter change in the active substance leads to a different mechanism of action that elevates dopamine levels in the eye, achieving myopia progression control without the rebound effects and adverse effects associated with atropine treatment

Inventive Principle:
Principle #35Parameter changes

4Quantity of substance

If levodopa is formulated in an aqueous carrier for ocular penetration, then intraocular dopamine levels are elevated, but formulation stability and solubility challenges must be overcome

Engineering Contradiction:
Improveintraocular dopamine levelsVSAvoidformulation stability
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The invention uses an aqueous carrier as an intermediary medium to deliver levodopa to ocular tissues. The aqueous formulation provides a stable and biocompatible vehicle that facilitates penetration through ocular barriers while maintaining levodopa solubility and stability, resolving the contradiction between achieving sufficient intraocular dopamine levels and ensuring formulation stability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the formulation parameter from potentially using organic solvents or complex delivery systems to a simple aqueous carrier. This parameter change in the solvent system achieves both adequate levodopa solubility and formulation stability, while facilitating ocular penetration and dopamine elevation

Inventive Principle:
Principle #35Parameter changes

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 compositions effectively inhibit the progression or development of visual disorders by elevating intraocular dopamine levels, offering a safer and more targeted treatment alternative to oral administration.

Implementation Method 1

aqueous formulations of levodopa in combination with an antioxidant can penetrate ocular tissues and significantly elevate intraocular dopamine levels

Methodology Applied
Scientific EffectPermeation: Permeation

Implementation Method 2

aqueous formulations of levodopa in combination with an antioxidant

Methodology Applied
Scientific EffectOxidation: Oxidation

Data Source

PatentEP4717276A2Ophthalmic compositions comprising levodopa, an antioxidant and an aqueous carrier
Publication Date: 2026.04.01 UNIVERSITY OF CANBERRA
  • EP4717276A2 patent drawingFigure 1
  • EP4717276A2 patent drawingFigure 2
  • EP4717276A2 patent drawingFigure 3

AI summary

Disclosed are compositions comprising levodopa and an antioxidant for inhibiting the development or progression of visual disorders inclusive of visual disorders associated with diabetic retinopathy or Parkinson's disease, and myopia.