Nanoemulsion Anti-Inflammatory Ocular Surface Relief
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Solution Overview
Problem
Current dry eye treatments, including artificial tears and anti-inflammatory drugs, are often ineffective or variably effective, and ophthalmic products face challenges with preservative use due to microbial growth concerns, especially in nanoemulsions which can clog filters during sterilization.
Innovation Solution
Development of a sterile-filtered oil-in-water nanoemulsion with oil globules of 100 nm or less, containing emulsion stabilizing polymers, surfactants, and tonicity modifiers, which exhibits anti-inflammatory activity without active pharmaceutical ingredients, allowing for effective ocular surface relief without preservatives.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If preservatives are used in ophthalmic products to prevent microbial growth, then microbial growth is prevented, but toxicity and irritation to the ocular surface increase
Solution Approach 1:
The patent removes preservatives from the ophthalmic composition entirely, extracting the harmful element while maintaining product functionality through sterile filtration and alternative preservation methods that do not harm the ocular surface
Solution Approach 2:
The patent employs single-use vials that are discarded after use, eliminating the need for long-term preservative systems. Each vial is sterile-filled and used once, then disposed of, avoiding cumulative exposure to preservative toxicity
2Reliability
If sterile filtration is applied to nanoemulsions to ensure sterility, then microbial contamination is prevented, but filter clogging occurs during the filtration process
Solution Approach 1:
The patent modifies the physical parameters of the nanoemulsion by controlling oil globule size to be within 0.01-10 micrometers and adjusting viscosity to 0.1-10 cP, allowing the formulation to pass through standard 0.22 micrometer filters without clogging while maintaining sterility
Solution Approach 2:
The patent performs sterile filtration as a preliminary step during manufacturing, establishing sterility before product use. The formulation is designed with appropriate rheological properties to enable successful filtration during production, ensuring sterility without requiring complex filtration processes
3Adaptability or versatility
If conventional artificial tears are used to replace tear film, then tear insufficiency is addressed, but anti-inflammatory activity is insufficient for severe dry eye disease
Solution Approach 1:
The patent creates a composite ophthalmic composition combining nanoemulsion technology with anti-inflammatory agents, integrating multiple functional components (tear film replacement, anti-inflammation, and controlled release) into a single formulation that addresses both tear insufficiency and inflammation simultaneously
4Reliability
If cationic preservatives are used in nanoemulsions to prevent microbial growth, then microbial growth is inhibited, but the nanoemulsion formulation becomes less stable and more irritating
Solution Approach 1:
The patent removes cationic preservatives from the formulation, extracting the element that causes instability and irritation. Instead, it employs non-cationic preservation strategies including sterile filtration and alternative agents that maintain nanoemulsion stability while preventing microbial growth
Solution Approach 2:
The patent changes the chemical parameters of the preservation system by switching from cationic to non-cationic or neutral preservatives, altering the electrostatic interactions that stabilize the nanoemulsion and eliminating the harmful effects of cationic irritation while maintaining microbial growth inhibition
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 nanoemulsion demonstrates anti-inflammatory activity comparable to or better than therapeutic compositions containing lifitegrast, providing effective relief for dry eye syndrome and other ocular surface disorders without the need for preservatives, as shown by improved corneal fluorescein staining scores.
Implementation Method 1
The nanoemulsion contains an oil, and at least one or more of emulsion stabilizing polymers, a water-soluble polymer, a surfactant, a tonicity modifier or stabilizer
Implementation Method 2
The nanoemulsion contains an oil, and at least one or more of emulsion stabilizing polymers, a water-soluble polymer, a surfactant
Implementation Method 3
The present invention relates to a sterile-filtered nanoemulsion having oil globules with a median size (Dv50) of about 100 nm or less
Data Source
AI summary
A sterile-filtered nanoemulsion having oil globules with a median size (Dv50) of about 100 nm or less and containing an oil, emulsion stabilizing polymer, a water-soluble polymer a surfactant, a tonicity modifier or stabilizer, or a combination thereof is provided. The nanoemulsion, even in the absence of an active ingredient, has ameliorative effects including anti-inflammatory activity. The present invention also provides a method of using such a nanoemulsion as an artificial tear composition for treating an ocular surface disorder, including those resulting from contact lens use, by administering an effective amount of the oil-in-water nanoemulsion of the present invention topically to an eye of a subject.