Niacinamide Oleic Acid Composition for Acne and Hyperpigmentation

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Solution Overview

Problem

Current treatments for acne and skin pigmentation disorders, such as those involving benzoyl peroxide, retinoids, azelaic acid, and antibiotics, are either ineffective as monotherapy or have limitations like rapid recurrence and skin cancer concerns, and there is a need for a composition that addresses both acne and hyperpigmentation effectively.

Innovation Solution

A topical composition combining niacinamide, oleic acid, and dimethylisosorbide, which acts synergistically to enhance anti-inflammatory and depigmenting properties, potentially including calamine and additional depigmenting agents like octadecenedioic acid or undecylenoyl phenylalanine, to treat acne and hyperpigmentation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If monotherapy with azelaic acid is used, then comedolytic and bacteriostatic effects are achieved, but anti-inflammatory effect is insufficient and treatment results are disappointing

Engineering Contradiction:
Improveanti-inflammatory effectVSAvoidtreatment effectiveness
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines azelaic acid with niacinamide and oleic acid in a single topical composition. This merging of multiple active ingredients allows the formulation to simultaneously provide comedolytic, bacteriostatic, and anti-inflammatory effects, resolving the limitation of azelaic acid monotherapy which lacked sufficient anti-inflammatory activity.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite dermatological composition integrating three distinct active compounds (azelaic acid, niacinamide, oleic acid) with complementary mechanisms of action. This composite approach enables the formulation to address multiple pathological factors of acne concurrently, achieving superior treatment effectiveness compared to monotherapy.

Inventive Principle:
Principle #40Composite materials

2Productivity

If topical retinoids are used, then acne treatment effectiveness is improved, but rapid recurrence occurs when treatment is stopped

Engineering Contradiction:
Improveacne treatment effectivenessVSAvoidduration of treatment effect
Core Design Contradiction:
ProductivityVSDuration of action of stationary object

Solution Approach 1:

The composition includes niacinamide, which normalizes keratinization and prevents follicular obstruction, and oleic acid, which has comedolytic properties. These ingredients continue to maintain skin health and prevent acne recurrence even after the treatment period ends, providing a lasting effect that mitigates the rapid recurrence problem associated with retinoids.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent uses azelaic acid at a specific concentration range (10-20%) optimized to provide sustained therapeutic effect. This parameter optimization ensures effective acne treatment while maintaining long-term benefits that prevent rapid recurrence upon discontinuation, addressing the duration limitation of conventional treatments.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If benzoyl peroxide is used, then acne treatment effect is achieved, but skin cancer risk is increased

Engineering Contradiction:
Improveacne treatment effectVSAvoidskin cancer risk
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent employs azelaic acid, a safer alternative to benzoyl peroxide, as the primary bacteriostatic and comedolytic agent. Azelaic acid provides effective acne treatment without the carcinogenic risks associated with benzoyl peroxide, offering a sustainable long-term treatment solution that does not compromise future skin health.

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

Solution Approach 2:

The invention uses oleic acid, which has inherent comedolytic and anti-inflammatory properties, to replace the harmful effects of benzoyl peroxide. Oleic acid effectively treats acne by dissolving comedones and reducing inflammation without inducing free radical damage or increasing skin cancer risk, thus converting the need for aggressive treatment into a safer therapeutic approach.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

4Productivity

If topical antibiotics are used, then acne treatment is effective, but resistance development and cosmetic usage restriction occur

Engineering Contradiction:
Improveacne treatment effectivenessVSAvoidcosmetic usage eligibility
Core Design Contradiction:
ProductivityVSAdaptability or versatility

Solution Approach 1:

The patent employs azelaic acid and niacinamide as non-antibiotic active ingredients that effectively treat acne without causing bacterial resistance. These ingredients are safe for long-term use and are permitted in cosmetic formulations, allowing the treatment to be used continuously for maintenance without the restrictions and resistance issues associated with topical antibiotics.

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

Solution Approach 2:

The invention replicates the therapeutic benefits of antibiotic treatment through alternative mechanisms. Azelaic acid provides bacteriostatic effects by inhibiting bacterial metabolism and protein synthesis, while niacinamide reduces inflammation and normalizes skin cell turnover. This copying of antibiotic efficacy through non-antibiotic pathways enables cosmetic usage without resistance development.

Inventive Principle:
Principle #26Copying

Data Source

PatentEP3151816B1Niacinamide-based dermatological composition
Publication Date: 2019.07.24 ESPA SA EXPERTS IN SCI & PROD ACHIEVEMENTS

AI summary

The present invention relates to a topical composition comprising: niacinamide, oleic acid and dimethyl isosorbide.