Non-ionic surfactant eye drops for dry eye treatment

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Solution Overview

Problem

Current treatments for dry eye syndrome, such as immunosuppressive agents, often cause significant side effects and have limited efficacy, making them undesirable for long-term use, especially in elderly patients, who are the primary affected demographic.

Innovation Solution

An ophthalmic composition containing a non-ionic surfactant, specifically polyoxyl 35 castor oil, is used in concentrations ranging from 0.01 to 8 weight/volume % to treat and prevent dry eye symptoms, providing rapid relief and improving ocular surface integrity with minimal side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If immunosuppressive agents are used to treat dry eye, then anti-inflammatory effect is improved, but side effects increase

Engineering Contradiction:
Improveanti-inflammatory effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the active ingredient from immunosuppressive agents to non-ionic surfactants, fundamentally altering the chemical parameter of the treatment. This substitution maintains therapeutic efficacy for dry eye while eliminating the severe side effects associated with immunosuppressants such as anemia, leukopenia, and thrombocytopenia

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs non-ionic surfactants which are safer, shorter-acting topical agents compared to systemic immunosuppressants. These surfactants provide localized treatment with minimal systemic absorption, effectively replacing long-term immunosuppressive therapy with safer, temporary topical applications

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Reliability

If immunosuppressive agents are used for severe dry eye, then treatment efficacy is improved, but patient compliance decreases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent transforms the treatment approach by using non-ionic surfactants with favorable safety profiles, enabling frequent administration without cumulative toxicity. This parameter change from immunosuppressants to surfactants allows elderly patients to maintain compliance while receiving effective treatment for severe dry eye

Inventive Principle:
Principle #35Parameter changes

3Reliability

If cyclosporine is applied to treat dry eye, then anti-inflammatory effect is improved, but cell viability decreases

Engineering Contradiction:
Improveanti-inflammatory effectVSAvoidcell viability
Core Design Contradiction:
ReliabilityVSStrength

Solution Approach 1:

The patent introduces non-ionic surfactants as intermediary substances that provide anti-inflammatory benefits without the direct cytotoxic effects of cyclosporine. These surfactants act as mediators between the need for inflammation control and the preservation of corneal epithelial cell viability, avoiding apoptosis and cell death

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces cyclosporine with non-ionic surfactants that are safer for cellular health. These surfactants provide temporary anti-inflammatory action without the severe cytotoxicity of cyclosporine, allowing repeated applications that preserve cell viability while treating inflammation

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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 composition significantly reduces dry eye symptoms and signs, as measured by SANDE scores, and improves ocular surface health, demonstrating a clinically significant improvement in both symptom relief and ocular surface integrity with a low incidence of side effects.

Implementation Method 1

an ophthalmic composition comprising a non-ionic surfactant as active ingredient

Methodology Applied
Scientific EffectSurface tension reduction: Surfactant

Implementation Method 2

a non-ionic surfactant is present in an effective amount from 0.01 to 8 weight/volume % based on the total composition

Methodology Applied
Scientific EffectEmulsion formation: Emulsion

Data Source

PatentEP3705114A1Ophthalmic composition for treating dry eye and symptoms thereof
Publication Date: 2020.09.09 ALCON INC
  • EP3705114A1 patent drawingFigure 1~1C
  • EP3705114A1 patent drawingFigure 2A~2B
  • EP3705114A1 patent drawing

AI summary

It is provided an ophthalmic composition, particularly formulated as eye drops, comprising a non-ionic surfactant as active ingredient, wherein the non-ionic surfactant is present in an effective amount from 0.01 to 8 weight/volume % based on the total composition, for use in treating or preventing dry eye and/or for relieving one or more symptoms and/or signs of dry eye. The ophthalmic composition exerts a rapid effect in treating dry eye symptoms and signs while having very low incidence of side effects.