Nitric Oxide-Releasing Composition for Inflammation Treatment

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Solution Overview

Problem

Current treatments for inflammatory skin conditions, such as psoriasis and atopic dermatitis, often rely on corticosteroids and biologics, which come with significant side effects, including cancer risks, and there is a need for a therapy that effectively addresses inflammation without these drawbacks.

Innovation Solution

A nitric oxide-releasing pharmaceutical composition comprising a diazeniumdiolate functional group is topically administered to the skin, mucosa, or eye, which includes a hydrophobic base, amphiphilic compound, emulsifying agent, water, buffering agent, polymer, and polyhydric alcohol, to treat inflammatory conditions by modulating inflammatory mediators and cytokines.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If corticosteroids are used to treat inflammatory skin conditions, then inflammation is effectively reduced, but long-term side effects and cancer risks increase

Engineering Contradiction:
Improveinflammation reduction effectivenessVSAvoidside effects and cancer risks
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameter of the treatment agent from corticosteroids to nitric oxide-releasing compounds (diazeniumdiolates). This parameter change maintains anti-inflammatory effectiveness while eliminating the harmful side effects associated with long-term corticosteroid use, including skin thinning, adrenal suppression, and cancer risks.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces nitric oxide as an intermediary molecule that mediates the anti-inflammatory effect. The diazeniumdiolate compounds serve as NO donors, releasing nitric oxide locally at the inflammation site to modulate inflammatory mediators and cytokines, thereby achieving anti-inflammatory effects without the systemic side effects of corticosteroids.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If biologics are used to treat inflammatory skin conditions, then severe inflammation is addressed, but severe side effects including cancer risks occur

Engineering Contradiction:
Improveinflammation treatment effectivenessVSAvoidsevere side effects and cancer risks
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs short-acting nitric oxide-releasing compounds that provide localized, transient anti-inflammatory effects. These compounds release nitric oxide on-demand and are metabolized quickly, avoiding the accumulation and severe long-term side effects associated with biologics, while still effectively addressing inflammation when needed.

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

Solution Approach 2:

The patent achieves local anti-inflammatory action through topically applied diazeniumdiolate compounds that release nitric oxide specifically at the site of inflammation. This local quality approach treats the affected area effectively while minimizing systemic exposure and associated severe side effects, including cancer risks, that are problematic with systemic biologics.

Inventive Principle:
Principle #3Local quality

3Object-affected harmful factors

If topical compositions are designed to release nitric oxide, then anti-inflammatory effects are achieved without systemic effects, but formulation complexity increases

Engineering Contradiction:
Improvesystemic effects eliminationVSAvoidformulation complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent employs composite topical formulations combining diazeniumdiolate compounds with appropriate pharmaceutical excipients, emulsifiers, and delivery vehicles. This composite approach enables controlled nitric oxide release at the application site while maintaining formulation stability and preventing systemic absorption, thereby achieving localized anti-inflammatory effects without the complexity of advanced delivery systems.

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 composition effectively decreases inflammation and inhibits key inflammatory cytokines, such as IL-17A, IL-17F, and IL-1β, without systemic effects, providing a potential alternative to traditional treatments with reduced side effects.

Implementation Method 1

a nitric oxide-releasing pharmaceutical composition comprising at least one nitric oxide releasing-compound comprising a diazeniumdiolate functional group

Methodology Applied
Scientific EffectNitric oxide release: Decomposition (biological)

Data Source

PatentUS10912743B2Compositions for treating inflammation and methods of treating the same
Publication Date: 2021.02.09 LIGAND PHARMACEUTICALS INC
  • US10912743B2 patent drawing
  • US10912743B2 patent drawing
  • US10912743B2 patent drawing

AI summary

Provided herein are compositions useful for treating inflammation in a subject and methods of decreasing inflammation in the skin, mucosa, and/or eye of a subject comprising applying a pharmaceutical composition that includes an NO-releasing compound to the skin, mucosa, and/or eye of the subject in an amount sufficient to decrease inflammation.