Ethosome Composition for Transdermal Delivery

Solution Overview

Problem

Ethosomes with high ethanol content have high transdermal absorption rates but cause skin irritation and have low drug encapsulation efficiency, making them unsuitable for cosmetic use, and reducing ethanol content increases nanoparticle size, reducing absorption rates.

Innovation Solution

A novel ethosome composition with optimized ethanol content (2-8 wt%) and a preparation method using high-pressure homogenization to maintain nanoparticle size and enhance encapsulation efficiency, incorporating a peptide-hydrogel complex to improve stability and skin delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If ethanol content in ethosomes is increased to achieve high transdermal absorption rate, then transdermal absorption rate is improved, but skin irritation increases and encapsulation efficiency decreases

Engineering Contradiction:

Improvetransdermal absorption rateVSAvoidskin irritation

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the ethanol content parameter to a specific range (5-20% by weight) rather than using high concentrations, thereby maintaining transdermal absorption enhancement while reducing skin irritation and improving encapsulation efficiency

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent combines ethanol with phospholipids and cholesterol to form a composite ethosome structure, where the synergistic interaction of these components achieves effective transdermal delivery with reduced ethanol concentration and minimized skin irritation

Inventive Principle:

Principle #40Composite materials

2Speed

If ethanol content in ethosomes is increased to achieve high transdermal absorption rate, then transdermal absorption rate is improved, but encapsulation efficiency decreases

Engineering Contradiction:

Improvetransdermal absorption rateVSAvoidencapsulation efficiency

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent optimizes the ethanol content parameter to a specific range (5-20% by weight) rather than using high concentrations, thereby maintaining transdermal absorption enhancement while reducing skin irritation and improving encapsulation efficiency

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent combines ethanol with phospholipids and cholesterol to form a composite ethosome structure, where the synergistic interaction of these components achieves effective transdermal delivery with reduced ethanol concentration and minimized skin irritation

Inventive Principle:

Principle #40Composite materials

3Object-affected harmful factors

If ethanol content is decreased to reduce skin irritation, then skin irritation is reduced, but nanoparticle size increases and transdermal absorption rate decreases

Engineering Contradiction:

Improveskin irritationVSAvoidtransdermal absorption rate

Core Design Contradiction:

Object-affected harmful factorsVSSpeed

Solution Approach 1:

The patent identifies and optimizes multiple parameters including ethanol content (5-20%), phospholipid concentration (0.1-10%), and cholesterol content (0.01-0.5%), where the combined optimization maintains small nanoparticle size and high absorption rate even at lower ethanol concentrations

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent combines ethanol with phospholipids and cholesterol to form a composite ethosome structure, where the synergistic interaction of these components achieves effective transdermal delivery with reduced ethanol concentration and minimized skin irritation

Inventive Principle:

Principle #40Composite materials

4Object-affected harmful factors

If ethanol content is decreased to reduce skin irritation, then skin irritation is reduced, but nanoparticle size increases

Engineering Contradiction:

Improveskin irritationVSAvoidnanoparticle size

Core Design Contradiction:

Object-affected harmful factorsVSVolume of moving object

Solution Approach 1:

The patent identifies and optimizes multiple parameters including ethanol content (5-20%), phospholipid concentration (0.1-10%), and cholesterol content (0.01-0.5%), where the combined optimization maintains small nanoparticle size and high absorption rate even at lower ethanol concentrations

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 solution achieves improved encapsulation efficiency and stability, reduces skin irritation, and maintains high transdermal absorption rates, making the ethosomes suitable for cosmetic use and suitable for mass-production.

Implementation Method 1

a preparation method using high-pressure homogenization to maintain nanoparticle size

Methodology Applied

Scientific EffectHigh-pressure homogenization: Compression

Implementation Method 2

it includes ethanol in order to have a higher transdermal absorption rate than a liposome, which provides reduced surface tension of phospholipids

Methodology Applied

Scientific EffectSurface tension reduction: Surfactant

Implementation Method 3

also imparts flexibility to the membrane of the vesicle itself

Methodology Applied

Scientific EffectMembrane flexibility: Elasticity

Data Source

PatentUS11452679B2Method of preparing bioactive substance-encapsulated ethosome, ethosome composition, and cosmetic composition including ethosome composition

Publication Date: 2022.09.27 BINOTEC CO LTD

AI summary

Provided is a method of preparing a bioactive substance-encapsulated ethosome, the method including: preparing an aqueous solution of a bioactive substance, preparing a lipid-dissolved solution by dissolving lipids in ethanol, preparing a hydrated liquid crystalline phase by hydrating the lipid-dissolved solution by mixing and agitating the bioactive substance aqueous solution together with the lipid-dissolved solution, and preparing an ethosome solution by adding purified water to the hydrated liquid crystalline phase to produce a mixture and agitating the mixture.