Nitric Oxide Releasing Compositions for Inflammatory Skin Conditions

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Solution Overview

Problem

Current treatments for inflammatory skin conditions and wounds face challenges in delivering therapeutic agents without irritating the skin and maintaining effectiveness, particularly with moisture-activated ingredients, as traditional aqueous vehicles can exacerbate inflammation and reduce the efficacy of active agents.

Innovation Solution

A pharmaceutical composition comprising a hydrophobic base, amphiphilic compound, moisture-activated active pharmaceutical ingredient, hydrophobic polymer, mineral oil, cosolvent, and humectant, designed for topical delivery to minimize moisture absorption and maintain the active ingredient's effectiveness while reducing irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If aqueous vehicles are used to deliver moisture-activated active ingredients, then the active ingredient can be delivered to the skin, but the aqueous vehicle exacerbates inflammation and reduces the efficacy of the active agent

Engineering Contradiction:
Improvedelivery of active ingredientVSAvoidinflammation and reduced efficacy
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical-chemical parameters of the vehicle system by transitioning from aqueous to anhydrous formulations. The composition uses a hydrophobic base (petrolatum, mineral oil, or silicone) combined with specific amphiphilic compounds to create a non-aqueous delivery system that maintains active ingredient stability while avoiding the inflammatory effects of water-based vehicles.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces amphiphilic compounds as intermediary substances that bridge the hydrophobic base and the moisture-activated active ingredient. These amphiphilic compounds facilitate the delivery and activation of the active agent without requiring aqueous environments, thereby eliminating the harmful inflammatory effects while maintaining delivery efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If mineral oil ointments are used to protect moisture-activated agents from moisture, then the active agent is protected prior to application, but the effectiveness of the active agent at the time of application is reduced

Engineering Contradiction:
Improveprotection of active agentVSAvoideffectiveness of active agent
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent applies local quality by using amphiphilic compounds that create different functional zones within the ointment structure. These compounds provide localized moisture regulation capabilities, allowing the ointment to protect the active agent during storage while enabling controlled moisture interaction at the application site to activate the agent without compromising its effectiveness.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent modifies the moisture-regulating parameters of the ointment by incorporating amphiphilic compounds that change the water activity and moisture distribution characteristics. This allows the system to maintain anhydrous protection during storage while providing controlled moisture activation at the skin interface, resolving the contradiction between protection and effectiveness.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If traditional aqueous vehicles are used for delivering therapeutic agents, then the active ingredient can be delivered, but substantial irritation is caused to the skin

Engineering Contradiction:
Improvedelivery of therapeutic agentVSAvoidskin irritation
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent fundamentally changes the vehicle parameters from aqueous to anhydrous formulations, eliminating water as the continuous phase. This parameter change removes the source of skin irritation associated with aqueous vehicles while maintaining the ability to deliver therapeutic agents through the hydrophobic base and amphiphilic compound system.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses amphiphilic compounds as intermediary delivery vehicles that facilitate the transport of therapeutic agents through the skin without requiring aqueous environments. These intermediaries provide a non-irritating delivery pathway that maintains agent efficacy while eliminating the skin irritation caused by traditional aqueous vehicles.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 delivers nitric oxide-releasing agents to treat inflammatory skin conditions and wounds, demonstrating bactericidal activity against Pseudomonas aeruginosa and Staphylococcus aureus, and showing anti-inflammatory and wound-healing properties without substantial irritation.

Implementation Method 1

an amphiphilic compound present in the composition at a concentration from about 1% to about 20%

Methodology Applied
Scientific EffectMoisture absorption: Absorption (physical)

Data Source

PatentUS11077194B2Nitric oxide releasing pharmaceutical compositions
Publication Date: 2021.08.03 LIGAND PHARMACEUTICALS INC
  • US11077194B2 patent drawing
  • US11077194B2 patent drawing
  • US11077194B2 patent drawing

AI summary

The present invention generally relates to nitric oxide releasing pharmaceutical compositions and methods of using the same.