Polymer-Phospholipid Topical Composition for Enhanced Skin Absorption

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Solution Overview

Problem

Topical administration of active ingredients is hindered by the skin's barrier effect, which limits the penetration and absorption of many active ingredients due to their low solubility and permeability.

Innovation Solution

A topical pharmaceutical composition comprising a cosmetically or pharmaceutically active substance, a polyvinylcaprolactam / polyvinyl acetate / polyethylene glycol copolymer (such as Soluplus), a hydrogenated phosphatidylcholine phospholipid, and a plasticizer at concentrations between 0.1% and 45% w/w, which enhances skin absorption by improving solubility and permeability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the skin's barrier function is maintained, then protection against pathogens and toxins is improved, but penetration and absorption of active ingredients deteriorates

Engineering Contradiction:

Improveskin barrier protectionVSAvoidtopical absorption of active ingredients

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs absorption promoters (penetration enhancers) as intermediary substances that facilitate the passage of active ingredients through the skin barrier. These promoters temporarily modify the skin's barrier properties to allow penetration, then restore it, thus mediating between the protective function and the need for ingredient delivery.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the active ingredients or the skin barrier environment (such as pH, temperature, or molecular structure) to enhance penetration while maintaining barrier integrity. This allows the skin to remain protective while permitting controlled absorption of therapeutic agents.

Inventive Principle:

Principle #35Parameter changes

2Ease of manufacture

If absorption promoters are added to enhance permeability, then skin penetration is improved, but solubility of active ingredients deteriorates

Engineering Contradiction:

Improveskin permeabilityVSAvoidsolubility of active ingredient

Core Design Contradiction:

Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent uses composite formulations combining multiple components including absorption promoters, solubility enhancers, and the active ingredient itself. This composite approach allows simultaneous improvement of permeability and maintenance of solubility through synergistic interactions between formulation components.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The invention modifies physical-chemical parameters such as pH, temperature, or molecular structure of the formulation components to simultaneously enhance both permeability and solubility. By adjusting these parameters, the formulation achieves optimal balance between penetration enhancement and ingredient stability.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If concentration of active ingredient is increased to improve efficacy, then treatment effectiveness is improved, but skin tolerability deteriorates

Engineering Contradiction:

Improvetreatment efficacyVSAvoidskin irritation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces absorption promoters and formulation excipients as intermediary substances that enable higher concentrations of active ingredients to be delivered without causing excessive irritation. These intermediaries protect the skin while facilitating enhanced therapeutic delivery.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the formulation (such as pH buffering, viscosity modification, or molecular size) to allow higher active ingredient concentrations to be tolerated by the skin. This enables improved efficacy while maintaining skin tolerability through parameter optimization.

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 achieves high levels of skin absorption for active ingredients, overcoming the skin's barrier effect and improving the efficacy of topical treatments for skin diseases and cosmetic applications.

Implementation Method 1

the addition of a polyvinylcaprolactam / polyvinyl acetate / polyethylene glycol copolymer to the combination of an active ingredient with phospholipids makes it possible to obtain aqueous solutions of active ingredients with a high level of skin absorption

Methodology Applied

Scientific EffectSolubility enhancement: Solvation

Implementation Method 2

substances that promote absorption (penetration enhancers) are commonly used, including phospholipids, which are known for their high skin tolerability

Methodology Applied

Scientific EffectPermeation enhancement: Permeation

Implementation Method 3

the addition of increasing concentrations of plasticisers improves the elongation characteristics of film containing Soluplus

Methodology Applied

Scientific EffectPlasticization:

Data Source

PatentEP3210595B1Pharmaceutical or cosmetic compositions comprising a polymer and an absorption promoter for controlled release of active ingredients

Publication Date: 2025.04.02 EMENEM SRL

Figure 1~2

AI summary

The present invention relates to a pharmaceutical or cosmetic composition or medical device for topical use comprising: a) a cosmetically or pharmaceutically active substance; b) a polyvinylcaprolactam / polyvinyl acetate / polyethylene glycol copolymer; c) a phospholipid.