Topical Composition for Acne via Nitric Oxide Release

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Solution Overview

Problem

Current skin treatments for acne vulgaris and inflammatory lesions are inadequate in effectively reducing P. acnes counts and lesion severity within a reasonable timeframe, often requiring longer periods for noticeable improvements.

Innovation Solution

A topical composition comprising a diluent, solvent, penetration enhancing agent, skin brightening agent, skin renewing agent, anti-irritant, pH adjustment agent, preservative, L-arginine, and L-citrulline, which includes an active pharmaceutical ingredient such as salicylic acid or a nitric oxide-releasing compound, applied therapeutically to the skin to enhance penetration and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional skin treatments are used for acne vulgaris and inflammatory lesions, then the treatments can be applied topically, but the reduction in P. acnes counts and lesion severity takes longer than a reasonable timeframe

Engineering Contradiction:
Improverate of lesion reductionVSAvoidtime to noticeable improvement
Core Design Contradiction:
ProductivityVSLoss of time

Solution Approach 1:

The patent modifies the chemical composition parameters of the topical treatment by incorporating specific active ingredients (L-arginine, L-citrulline, nitric oxide-releasing compounds, salicylic acid) at optimized concentrations to accelerate the reduction of P. acnes and lesions while maintaining safety

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses composite formulations combining multiple active ingredients working synergistically - nitric oxide-releasing compounds, amino acids (L-arginine, L-citrulline), salicylic acid, and supporting agents - to achieve faster and more effective acne treatment than single-component treatments

Inventive Principle:
Principle #40Composite materials

2Productivity

If stronger active ingredients are used to reduce P. acnes and lesions faster, then the effectiveness improves, but skin irritation and tolerability worsen

Engineering Contradiction:
Improverate of P. acnes reductionVSAvoidskin irritation
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent employs intermediary substances such as L-arginine, L-citrulline, and amino acid derivatives that serve as carriers or modulators, enabling the delivery of active ingredients like nitric oxide-releasing compounds and salicylic acid while buffering their potential irritant effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation optimizes the concentration parameters of active ingredients and supporting agents to achieve the minimum effective dose for P. acnes reduction while staying below irritation thresholds, creating a balanced therapeutic window

Inventive Principle:
Principle #35Parameter changes

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 reduces inflammatory and non-inflammatory lesions by 10% or greater and P. acnes counts within 12 weeks or less, often achieving results in 8 weeks or less, with improved tolerability and reduced skin irritation compared to existing treatments.

Implementation Method 1

L-arginine and L-citrulline have been shown to convert nitrate to nitric oxide in skin cells, releasing nitric oxide that can reduce P. acnes and inflammatory lesions

Methodology Applied
Scientific EffectNitric oxide release:

Implementation Method 2

A penetration enhancing agent may be present in the composition. The penetration enhancing agent may enhance penetration of the composition through the skin

Methodology Applied
Scientific EffectPenetration enhancement: Permeation

Data Source

PatentUS11534382B2Topical compositions and methods of using the same
Publication Date: 2022.12.27 LIGAND PHARMACEUTICALS INC

AI summary

The present invention relates generally to compositions and methods of using the same such as, for example, methods of treating the skin of a subject using a composition as described herein. The composition may comprise a diluent, a solvent, a penetration enhancing agent, a skin brightening agent, a skin renewing agent, a thickening agent, an anti-irritant, a chelating agent, an active pharmaceutical ingredient (API), optionally a pH adjustment agent, and optionally a preservative. The composition may further comprise L-arginine and/or L-citrulline and/or esters and/or derivatives thereof.