Preservative-Free Microemulsion for Dry Eye Treatment

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Solution Overview

Problem

Current ophthalmic compositions for treating dry eye syndrome often contain irritating ionic surfactants and preservatives, leading to potential eye irritation and low patient compliance, while existing treatments with active agents like cyclosporine A or lifitegrast may cause side effects and have limited long-term efficacy.

Innovation Solution

A microemulsion comprising an oily component, an aqueous phase, a non-ionic surfactant, a polysaccharide, and a cross-linking agent, which avoids the use of ionic compounds and preservatives, providing improved shelf-life, wetting, and ocular tolerability, and is free from harmful ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If ionic surfactants and preservatives are used in ophthalmic compositions, then emulsion stability and shelf-life are improved, but eye irritation and harmful effects increase

Engineering Contradiction:
Improveemulsion stabilityVSAvoideye irritation
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent removes ionic surfactants and preservatives from the ophthalmic composition, extracting the harmful components while maintaining the therapeutic function through alternative non-ionic surfactant systems

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces non-ionic surfactants as intermediary substances that provide the necessary emulsion stability and shelf-life without causing eye irritation, serving as a safe mediator between the oily and aqueous phases

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If active agents like cyclosporine A or lifitegrast are used for severe DES treatment, then treatment efficacy is improved, but side effects and low patient compliance increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs a simple, preservative-free microemulsion formulation that can be used frequently without accumulating harmful effects, replacing long-term drug therapy with a safer, repeatable topical application

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

Solution Approach 2:

The patent changes the physical state and delivery mechanism of therapeutic components by using a microemulsion system with optimized droplet size and composition, improving penetration and efficacy while reducing the need for high-dose pharmaceutical agents

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If conventional emulsions are used for dry eye treatment, then basic lubrication is provided, but wetting properties and ocular tolerability are insufficient

Engineering Contradiction:
Improvelubrication functionVSAvoidocular tolerability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent creates a composite microemulsion system combining oily components, aqueous phase, non-ionic surfactants, and polysaccharides in specific ratios, achieving superior wetting properties and ocular tolerability that individual components cannot provide alone

Inventive Principle:
Principle #40Composite materials

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 microemulsion effectively treats dry eye syndrome by enhancing tear film reconstruction, reducing water evaporation, and lubricating the ocular surface, while maintaining stability and avoiding eye irritation, thus offering a more tolerable and effective treatment option compared to existing formulations.

Implementation Method 1

at least one non-ionic surfactant

Methodology Applied
Scientific EffectSurface tension reduction: Surfactant

Implementation Method 2

at least one cross-linking agent

Methodology Applied
Scientific EffectCross-linking: Chemical Bonding

Implementation Method 3

improved shelf-life

Methodology Applied
Scientific EffectStabilization:

Implementation Method 4

reducing water evaporation

Methodology Applied
Scientific EffectEvaporation reduction: Evaporation

Data Source

PatentUS20230355522A1Microemulsion for the treatment of dry eye syndrome
Publication Date: 2023.11.09 AZAD PHARMA
  • US20230355522A1 patent drawing
  • US20230355522A1 patent drawing
  • US20230355522A1 patent drawing

AI summary

The present invention refers to a microemulsion, particularly suitable for ophthalmic applications such as treatment of dry eye syndrome, which comprises at least one oily component, an aqueous phase, at least one non-ionic surfactant, at least one polysaccharide, a salt or a derivative thereof, and at least one cross-linking agent. Moreover, the present invention relates to a process of manufacturing a microemulsion according to the invention, as well as its use in ophthalmic applications or as a carrier.