Fatty Amine Core-Shell Nanoparticles for Transdermal CSSC Delivery

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Solution Overview

Problem

Conventional methods for delivering cosmeceuticals and pharmaceuticals topically face challenges such as residual volatile organic compounds (VOCs) causing toxicity, altered particle structure, and inefficient skin penetration of high molecular weight molecules, leading to incomplete delivery and potential skin damage.

Innovation Solution

Development of core-shell nano-elements with a water-insoluble collagen-synthesis stimulating compound (CSSC) and a fatty amine shell, dispersed in a polar carrier, which allows for stable, non-covalent association and reduced viscosity, facilitating transdermal delivery of high molecular weight molecules.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional topical delivery methods are used, then application simplicity is maintained, but skin penetration efficiency deteriorates due to molecular weight limitations

Engineering Contradiction:
Improveapplication simplicityVSAvoidskin penetration efficiency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent segments large collagen molecules into smaller peptide fragments (e.g., 2-10 kDa molecular weight) that can penetrate skin while maintaining structural integrity. This segmentation allows topical application to effectively deliver collagen-building components through the skin barrier, resolving the contradiction between application simplicity and penetration efficiency.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent changes the molecular weight parameter of collagen from full-length (100-300 kDa) to optimized fragments (2-10 kDa), enabling transdermal penetration while preserving biological activity. This parameter modification allows conventional topical delivery to effectively reach deeper skin layers.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If high molecular weight collagen is used, then biological activity is improved, but transdermal delivery efficiency deteriorates

Engineering Contradiction:
Improvebiological activityVSAvoidtransdermal delivery efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

Collagen is segmented into peptide fragments containing specific amino acid sequences (e.g., Gly-Pro-Hyp repeats) that maintain collagen-triple-helix formation capability and biological activity while reducing molecular weight to 2-10 kDa for effective transdermal delivery.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates composite peptide structures combining collagen-derived sequences with penetration-enhancing moieties, achieving both high biological activity and improved transdermal delivery efficiency through molecular design.

Inventive Principle:
Principle #40Composite materials

3Ease of manufacture

If volatile organic compounds are used in nano-particle preparation, then manufacturing process is simplified, but skin toxicity increases

Engineering Contradiction:
Improvemanufacturing process simplicityVSAvoidskin toxicity
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent changes the solvent parameter from volatile organic compounds to water or alcohol-based aqueous systems, eliminating toxic residue concerns while maintaining nano-particle formation capability through modified preparation protocols.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses water as an inert, non-toxic medium for nano-particle synthesis and stabilization, replacing volatile organic solvents to create biocompatible collagen peptide formulations suitable for topical skin application.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

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 effective transdermal delivery of CSSCs and active agents with reduced toxicity and improved skin penetration, enabling higher concentrations and molecular weights, while maintaining their biological activity.

Implementation Method 1

a shell of at least one fatty amine surrounding the core, the fatty-amine(s) non-covalently interacting with the CSSC

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Implementation Method 2

The core-shell nano-elements may be further stabilised by the presence of at least one surfactant in the polar carrier in which the core-shell nano-elements are dispersed

Methodology Applied
Scientific EffectSteric stabilization:

Implementation Method 3

facilitating transdermal delivery of high molecular weight molecules

Methodology Applied
Scientific EffectTransdermal penetration: Permeation

Data Source

PatentEP4536755B1Compositions comprising surface modified globular nano-particles
Publication Date: 2026.02.25 LANDA LABS 2012
  • EP4536755B1 patent drawingFigure 1
  • EP4536755B1 patent drawingFigure 2~3
  • EP4536755B1 patent drawingFigure 4

AI summary

There are disclosed compositions comprising core-shell nano-elements composed in their core of a water-insoluble thermoplastic compound having a molecular weight of more than 0.6 kDa and in their shell of at least one fatty amine, or a part thereof, the core-shell nano-elements having a viscosity of 107 mPa·s or less and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less. The water-insoluble thermoplastic compound can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon application of the core-shell nano-elements to a surface to be treated therewith. Methods for preparing the composition and uses thereof are also provided.