Tetrapeptide-Functionalized Microcapsules for Skin Penetration

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Solution Overview

Problem

Existing methods for enhancing skin penetration of substances through the epidermis are inefficient and often require high doses, leading to potential side effects.

Innovation Solution

Development of microcapsules with a polymeric shell functionalized by covalent coupling of specific peptides, such as D-Arg-Tyr-Orn-Phe-NH2, Lys-Phe-Asn-Leu-Pro-Ala-Gly-Asn-Tyr-Lys-Pro-NH2, and Lys-Thr-Thr-Lys-Ser-OH, which enhance skin penetration and provide controlled release of encapsulated active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If classical penetration enhancers (isopropyl myristate, decyl oleate, etc.) are used to accelerate passage through stratum corneum, then skin penetration is improved, but side effects increase and high doses are required

Engineering Contradiction:

Improveskin penetration rateVSAvoidside effects

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent introduces peptide-functionalized polymeric microcapsules as intermediary carriers that facilitate skin penetration without requiring high doses of classical penetration enhancers. The microcapsules encapsulate active substances and deliver them through the skin barrier, with the peptide functionalization enabling targeted interaction with skin structures, thereby reducing side effects while maintaining effective penetration.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical and physical parameters of the delivery system by using biodegradable polymeric microcapsules with peptide functionalization instead of classical penetration enhancers. This parameter change enables controlled release and targeted delivery, improving penetration efficiency at lower doses and reducing harmful side effects.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If high doses of active ingredients are used to achieve effective penetration, then penetration efficacy is improved, but side effects increase

Engineering Contradiction:

Improvepenetration efficacyVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the active ingredient into microcapsule units, each containing a controlled amount of the substance. This segmentation allows for precise dosing and controlled release, ensuring effective penetration without requiring high overall doses, thereby reducing side effects while maintaining reliability of the penetration effect.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The microcapsule system provides continuous controlled release of the active ingredient through the skin, maintaining effective concentrations at the target site over time. This continuous action improves penetration reliability without requiring high initial doses, thereby reducing side effects.

Inventive Principle:

Principle #20Continuity of useful action

3Duration of action of moving object

If polymeric microcapsules are used for encapsulation and targeted delivery, then controlled release is improved, but manufacturing complexity increases

Engineering Contradiction:

Improvecontrolled release durationVSAvoidmicrocapsule structure

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent uses polymeric microcapsules that serve multiple functions: encapsulation of active ingredients, targeted delivery to skin, controlled release over time, and reduced side effects. This multi-functionality justifies the increased structural complexity by providing sustained controlled release and improved therapeutic outcomes through a single integrated system.

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 microcapsules demonstrate higher skin-penetration and uniform distribution, reducing the amount of active ingredients needed and minimizing side effects while providing sustained release.

Implementation Method 1

functionalized by covalent coupling of a specific first peptide of formula (I) and a second peptide selected from the group consisting of peptide (II) and peptide (III)

Methodology Applied

Scientific EffectCovalent coupling: Chemical Bonding

Implementation Method 2

The penetration of substances through the epidermis is one of the challenges for developers of topical products designed for the dermal delivery of active substances through the skin

Methodology Applied

Scientific EffectSkin penetration: Permeation

Implementation Method 3

chemically stable biodegradable delivery vehicles that can release active substances at the targeted tissue or area

Methodology Applied

Scientific EffectControlled release: Diffusion

Data Source

PatentUS12440430B2Use of tetrapeptides and functionalised microcapsules as skin penetration carriers

Publication Date: 2025.10.14 EVONIK OPERATIONS GMBH

AI summary

Microcapsules contain a peptide (I), and peptides (II) or (III) coupled to a PLGA-containing polymeric shell. The microcapsules can be used to enhance skin penetration of active ingredients encapsulated therein, particularly in the field of cosmetics. A process can be used for preparing the microcapsules, and compositions can contain said microcapsules. The microcapsules can be used as a transdermal delivery system for the active ingredients encapsulated therein.