Eutectic Glycol Formulation for Rapid Skin Permeation

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Solution Overview

Problem

Current compositions for delivering cosmetic and pharmaceutical agents through the skin face challenges in achieving rapid absorption, non-greasy appearance, and effective penetration, while maintaining skin integrity and avoiding irritation.

Innovation Solution

A composition comprising biocompatible organic solvents, a polar lipid, surfactant, water, urea, and a thickener, with specific ratios and pH adjustment, to enhance the delivery of active agents through the skin, ensuring rapid absorption and pleasant application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional vehicles or carriers are used for percutaneous delivery, then the formulation can be applied topically, but the rate of percutaneous delivery of pharmaceutical active is significantly decreased

Engineering Contradiction:
Improverate of percutaneous deliveryVSAvoidpenetration effectiveness
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent changes the chemical parameters of the delivery vehicle by using a eutectic mixture of glycols (propylene glycol and ethylene glycol) instead of conventional carriers. This parameter change creates a formulation that effectively penetrates the stratum corneum barrier, resolving the contradiction between topical applicability and penetration effectiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs a composite delivery system combining multiple components: eutectic glycol mixture, water-soluble penetration enhancer, surfactant, and active agent. This composite formulation works synergistically to achieve both topical applicability and effective percutaneous penetration, overcoming the limitations of single-component conventional carriers.

Inventive Principle:
Principle #40Composite materials

2Speed

If penetration enhancers are used to increase absorption rate, then the active agent penetrates skin faster, but skin irritation and damage to skin integrity may occur

Engineering Contradiction:
Improveabsorption rateVSAvoidskin irritation
Core Design Contradiction:
SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent uses a water-soluble penetration enhancer and adjusts the pH of the formulation to optimize penetration while minimizing irritation. By changing the solubility and pH parameters, the formulation achieves rapid absorption without compromising skin integrity or causing significant irritation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces a surfactant as an intermediary component that facilitates the delivery of the active agent through the skin barrier. The surfactant acts as a mediator between the hydrophilic active agent and the lipophilic stratum corneum, enabling penetration without requiring harsh penetration enhancers that would cause skin irritation.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If multiple components are combined to achieve rapid penetration and pleasant appearance, then the formulation performance is improved, but the formulation complexity increases

Engineering Contradiction:
Improveformulation performanceVSAvoidformulation complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent merges multiple functions into a single integrated formulation system. The eutectic glycol mixture serves as both the penetration-enhancing vehicle and the base carrier, while the surfactant simultaneously provides solubilization and penetration enhancement. This merging reduces the need for separate complex components while maintaining high formulation performance.

Inventive Principle:
Principle #5Merging (Combining)

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 enables rapid and effective permeation of active agents across the skin, providing local therapeutic benefits with minimal skin irritation and a pleasant application experience, outperforming existing formulations in terms of absorption and efficacy.

Implementation Method 1

the vehicle or carrier aids in, or at a minimum does not adversely affect, the penetration of the selected active agent

Methodology Applied
Scientific EffectPercutaneous absorption: Permeation

Implementation Method 2

The organic solvents comprise an ester and a dihydric and/or polyhydric alcohol

Methodology Applied
Scientific EffectEutectic mixture effect:

Implementation Method 3

a polar lipid, at least one surfactant

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Implementation Method 4

allows the formulation with the agent(s) to be rapidly absorbed through the skin

Methodology Applied
Scientific EffectWetting: Wetting

Implementation Method 5

water, urea and a thickener

Methodology Applied
Scientific EffectThickening:

Implementation Method 6

to have a pleasing, non-greasy, non-oily appearance and feel

Methodology Applied
Scientific EffectViscosification:

Data Source

PatentUS7740875B2Organo-gel formulations for therapeutic applications
Publication Date: 2010.06.22 MQT HOLDINGS LLC

AI summary

A composition suitable for the local delivery of cosmetic and/or pharmaceutical agents into the skin containing at least two biocompatible organic solvents, a polar lipid, a surfactant, water, urea and a thickener wherein the organic solvents include an ester and a dihydric and/or polyhydric alcohol is provided. Also disclosed are compositions that further contain a cosmetic and/or pharmaceutical agent, along with the preparation and use thereof.