Topical IL-1Ra Composition for Ocular Inflammation

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Solution Overview

Problem

Current treatments for ocular and adnexal tissue inflammation, such as blepharitis, face challenges including long-term side effects from steroids, drug resistance with antibiotics, and insufficient persistence at the target site for signaling inhibitors, leading to systemic complications.

Innovation Solution

A topical composition comprising IL-1 antagonists or a combination of IL-1 and other inflammatory antagonists is administered to locally inhibit inflammation in ocular and adnexal tissues, using formulations like eye drops, ointments, or gels, which directly target the affected area without systemic dissemination.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If systemic drugs (steroids, antibiotics, immune-system inhibitors) are administered to treat ocular inflammation, then anti-inflammatory effect is achieved, but long-term side effects occur (damaging effects from steroids, drug resistance from antibiotics, insufficient persistence from signaling inhibitors)

Engineering Contradiction:
Improveanti-inflammatory effectVSAvoidlong-term side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent divides the treatment approach by using topical administration to deliver anti-inflammatory agents directly to the ocular surface, segmenting the systemic treatment into localized therapy. This allows the anti-inflammatory effect to be achieved at the target site while avoiding systemic circulation and associated long-term side effects.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by formulating compositions for topical ocular administration that concentrate the anti-inflammatory activity precisely where needed (ocular surface and adnexal tissues). This localized delivery ensures high efficacy at the treatment site while minimizing exposure of other body systems to the drugs, thereby reducing long-term side effects.

Inventive Principle:
Principle #3Local quality

2Reliability

If systemic immune-system inhibitors are administered to treat ocular inflammation, then inflammation is suppressed, but susceptibility to additional complications increases

Engineering Contradiction:
Improveinflammation suppressionVSAvoidsusceptibility to complications
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the immune suppression effect by using topical administration to confine the anti-inflammatory action to the ocular surface. This localized approach suppresses inflammation where needed while avoiding systemic immune suppression that would increase susceptibility to other complications.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements local quality by delivering immune-modulating agents topically to the eye, creating a localized anti-inflammatory environment without affecting the systemic immune system. This ensures inflammation suppression at the target site while maintaining overall immune competence and reducing susceptibility to additional complications.

Inventive Principle:
Principle #3Local quality

3Object-affected harmful factors

If topical composition is administered to locally treat ocular inflammation, then systemic side effects are minimized, but drug absorption and persistence at target site must be optimized

Engineering Contradiction:
Improvesystemic side effectsVSAvoidpersistence at target site
Core Design Contradiction:
Object-affected harmful factorsVSDuration of action of moving object

Solution Approach 1:

The patent applies parameter changes by optimizing the formulation parameters of the topical composition, including pH, osmolarity, viscosity, and incorporation of penetration enhancers or sustained-release vehicles. These parameter adjustments improve drug persistence at the ocular surface while maintaining minimal systemic absorption, thus balancing local efficacy with reduced systemic side effects.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS10105441B2Method for inhibiting or reducing dry eye disease by IL-1Ra
Publication Date: 2018.10.23 SCHEPENS EYE RESEARCH INSTITUTE INC
  • US10105441B2 patent drawing
  • US10105441B2 patent drawing
  • US10105441B2 patent drawing

AI summary

The present invention comprises a composition with means to inhibit the function of the inflammatory cytokine IL-1 and methods for using this composition to treat inflammatory disease of ocular and adnexal tissues by topical administration. The present invention also discloses devices for delivering this composition to target tissues.