Antimicrobial Phospholipid Complexes for Scalp Substantivity

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Solution Overview

Problem

Current antidandruff agents are not sufficiently substantive to the scalp and hair, often separate in aqueous shampoos due to density mismatch, leading to instability and reduced efficacy, and many have cytotoxic potential or cause irritation, with limited effectiveness against Malassezia yeasts and instability at natural scalp pH.

Innovation Solution

Development of water-soluble synthetic phospholipids with two undecylenic acid moieties and their synergistic combinations with sophorolipids, which are cosmetically compatible, stable at natural pH, and provide broad-spectrum antimicrobial activity, enhancing substantivity and reducing irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If water-insoluble particulate antidandruff agents are used, then antimicrobial activity against Malassezia yeasts is achieved, but the agents separate from aqueous shampoo base due to density mismatch, leading to compositional instability

Engineering Contradiction:
Improveantimicrobial activityVSAvoidcompositional stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the solubility parameter of the antidandruff agent by using water-soluble phospholipid complexes containing undecylenic acid and zinc pyrithione. This allows the active ingredients to remain dissolved in the aqueous shampoo base, eliminating separation issues while maintaining antimicrobial efficacy against Malassezia yeasts.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite water-soluble phospholipid complex that combines multiple functional components: phospholipids as the carrier matrix, undecylenic acid for antifungal activity, and zinc pyrithione for enhanced antimicrobial effect. This composite structure provides both stability in aqueous media and reliable antimicrobial action.

Inventive Principle:
Principle #40Composite materials

2Reliability

If water-insoluble particulate antidandruff agents are used, then antimicrobial activity is achieved, but the agents aggregate in aqueous cosmetic products, decreasing available surface area and resulting in loss of antidandruff activity

Engineering Contradiction:
Improveantimicrobial activityVSAvoidavailable surface area
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the physical state parameter of the antidandruff agent from particulate solid to water-soluble molecular complex. The phospholipid-based soluble complexes maintain individual molecules dispersed in the aqueous phase, preventing aggregation and maximizing the available surface area for antimicrobial action.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional antidandruff actives are used at higher concentrations to achieve better dandruff reduction, then antimicrobial efficacy is improved, but cytotoxic potential and skin irritation increase

Engineering Contradiction:
Improvedandruff reduction efficacyVSAvoidcytotoxic potential
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical nature of the active agent by using biocompatible phospholipid complexes that mimic natural skin lipids. This allows effective antimicrobial activity against Malassezia at lower concentrations without the cytotoxic effects associated with conventional synthetic antifungals, as the phospholipid structure is inherently gentle on skin cells.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The phospholipid complex acts as an intermediary carrier that delivers the antimicrobial active ingredients (undecylenic acid and zinc pyrithione) to the target Malassezia yeasts while protecting skin cells from direct contact with potentially cytotoxic substances. The phospholipid membrane structure provides selective permeability.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Duration of action of stationary object

If antidandruff actives are made substantive to extend efficacy from one shampoo treatment to the next, then long-term effectiveness is achieved, but the actives may not be compatible with cosmetic ingredients and difficult to formulate

Engineering Contradiction:
ImprovesubstantivityVSAvoidformulation compatibility
Core Design Contradiction:
Duration of action of stationary objectVSEase of manufacture

Solution Approach 1:

The phospholipid complex structure provides multi-functionality: it serves as the antimicrobial active delivery system, provides substantivity to hair and scalp through phospholipid binding, maintains compatibility with cosmetic ingredients due to its natural lipid structure, and ensures stability in aqueous formulations. This single molecular structure accomplishes multiple functions simultaneously.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 compounds demonstrate greater than 99.9% killing of Malassezia furfur within five minutes, are stable and effective at natural scalp pH, non-irritant, and maintain long-term substantivity, offering superior antidandruff activity and compatibility with cosmetic ingredients.

Implementation Method 1

The compounds demonstrate greater than 99.9% killing of Malassezia furfur within five minutes

Methodology Applied
Scientific EffectAntimicrobial activity:

Implementation Method 2

synthetic phospholipids which can be used as an antifungal agent

Methodology Applied
Scientific EffectCell membrane disruption:

Implementation Method 3

stable and effective at natural pH of the scalp or skin (i.e., pH 4.0-5.0)

Methodology Applied
Scientific EffectpH stability:

Implementation Method 4

highly substantive, scalp & skin compatible

Methodology Applied
Scientific EffectHydrophobic interaction:

Implementation Method 5

maintain long-term substantivity

Methodology Applied
Scientific EffectVan der Waals force: Van der Waals Force

Implementation Method 6

synergistic combinations of phospholipids of formula I with sophorolipids of formula II

Methodology Applied
Scientific EffectSynergistic effect:

Implementation Method 7

broad-spectrum antimicrobial activity

Methodology Applied
Scientific EffectMembrane permeabilization:

Data Source

PatentUS11771634B2Antimicrobial antifungal composition
Publication Date: 2023.10.03 GODREJ INDUSTRIES LTD
  • US11771634B2 patent drawing
  • US11771634B2 patent drawing
  • US11771634B2 patent drawing

AI summary

A synergistic antimicrobial composition for use in personal care products functions as an antifungal agent in hair shampoo and hair care products, and includes (A) an undecylenic acid based phosphobetaine depicted by Formula I, where R=Undecylenic acid:and (B) a sophorolipid, a biosurfactant produced by a fermentation process using Candida bombicola, having a structure as depicted by Formula II(A), Formula II(B), or a mixture thereof: