Ophthalmic Microemulsion Formulation for Dry Eye Lubrication

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for dry eye disease (DED) are often costly, have mixed efficacy, and can cause ocular burning, leading to patient discomfort and inadequate relief from chronic symptoms.

Innovation Solution

The development of ophthalmic pharmaceutical formulations that include lubricity-promoting ingredients, surfactants, mucoadhesive polymers, osmoprotectants, and nutritional components such as amino acids and vitamins, formulated as microemulsions or nanoemulsions to enhance ocular health, improve eye comfort, and facilitate the delivery of pharmacological agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional prescription products are used to treat dry eye disease, then some therapeutic effect may be achieved, but patient discomfort increases due to ocular burning and high cost

Engineering Contradiction:
Improvetherapeutic effectVSAvoidocular burning
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention uses composite lipid materials combining multiple lipid types (cholesterol, phospholipids, free fatty acids, triglycerides) with specific ratios to create a tear film substitute that mimics natural tears more closely, reducing ocular burning while maintaining therapeutic effectiveness

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The invention optimizes specific parameters including lipid composition ratios, osmolarity (280-320 mOsm/L), pH (6.5-7.5), and viscosity to match physiological conditions, thereby reducing ocular burning sensation while preserving therapeutic action

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If conventional tear substitutes are used, then some relief from dryness is provided, but visual blurring occurs reducing patient comfort

Engineering Contradiction:
Improvedryness reliefVSAvoidvisual clarity
Core Design Contradiction:
Object-affected harmful factorsVSIllumination intensity

Solution Approach 1:

The invention carefully controls viscosity parameters and lipid particle size distribution to ensure the formulation remains optically clear while providing adequate lubrication, eliminating visual blurring while maintaining dryness relief

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The formulation provides different functional properties in different phases: the aqueous phase maintains optical clarity for vision, while the lipid microemulsion droplets provide lubrication and dryness relief, achieving local quality differentiation

Inventive Principle:
Principle #3Local quality

3Object-affected harmful factors

If lubricating agents are applied to relieve dry eye symptoms, then comfort is improved, but the complexity of the formulation increases

Engineering Contradiction:
ImprovecomfortVSAvoidformulation complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The lipid microemulsion system performs multiple functions simultaneously: lubrication, tear film stabilization, drug delivery vehicle, and osmotic balance, reducing the need for separate formulation components and simplifying the overall formulation complexity

Inventive Principle:
Principle #6Universality (Multi-functionality)

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

These formulations provide effective relief from dry eye symptoms by improving lubrication, reducing discomfort, and promoting corneal health, while also serving as a platform for delivering active agents to treat ocular conditions with enhanced patient comfort and reduced visual blurring.

Implementation Method 1

the ophthalmic pharmaceutical formulations are in the form of a microemulsion or nanoemulsion formed from lipids and/or natural plant oils and surfactants

Methodology Applied
Scientific EffectMicroemulsion: Microemulsion

Implementation Method 2

surfactant(s) that solubilize lipid and/or plant oil ingredient(s) and assist in lubrication, and assist in easily spreading over hydrophobic surfaces

Methodology Applied
Scientific EffectSurfactant: Surfactant

Implementation Method 3

mucoadhesive polymer(s) that demonstrate shear thinning flow behavior

Methodology Applied
Scientific EffectShear thinning: Shear Thinning

Implementation Method 4

osmoprotectants. In some embodiments, the same ingredient can provide the effects of one or more of the lubricity-promoting ingredient(s), surfactant(s), lipid and/or plant oil ingredient(s), and/or mucoadhesive polymer(s)

Methodology Applied
Scientific EffectOsmoprotection: Osmotic Pressure

Data Source

PatentUS11951123B2Fortified nutritional lubricating drops for dry eye disease
Publication Date: 2024.04.09 PLATFORM OPHTHALMIC INNOVATIONS LLC

AI summary

The invention describes ophthalmic pharmaceutical formulations comprising pharmaceutical ingredients to address DED symptoms. In one aspect of the invention, an ophthalmic pharmaceutical formulation comprises: 1) lubricity-promoting ingredient(s) such as those listed in the FDA over the counter (OTC) monograph for ophthalmics as demulcents and 2) surfactant(s) that solubilize lipids, assist in lubrication, and assist in easily spreading over hydrophobic surfaces; and/or 3) lipid and/or plant oil ingredient(s) that assist in film formation and the spreading of tear fluid while promoting (or at least not inhibiting) lubrication; and/or 4) mucoadhesive and viscosity promoting polymer(s) that demonstrate shear thinning flow behavior. The pharmaceutical ingredients and osmoprotectant/tonicity ingredients are combined with ingredients that provide direct to the eye nutritional support that is comprehensive in nature. The total nutritional approach uses metabolically important tear fluid amino acids, vitamins, and both fatty acids/triglycerides and sugar molecules as energy sources. The invention results in both improved eye health and improved dry eye patient comfort.