Cyclodextrin COF–Polymer Composite for Stable Skin Penetration

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Solution Overview

Problem

Existing technologies face challenges in efficiently delivering active ingredients through the skin in a stable manner due to the skin's barrier function, particularly the stratum corneum, which limits the penetration of substances larger than 100 to 200 nm.

Innovation Solution

A composite is developed comprising a cyclodextrin-based covalent organic framework (CD-COF) and a polymer, formed through a method involving dissolution, crystallization using a gas diffusion crystallizer, and subsequent washing and drying, to enhance transdermal delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the stratum corneum barrier function is maintained, then skin protection is improved, but active ingredient penetration is worsened

Engineering Contradiction:

Improveskin protectionVSAvoidactive ingredient penetration

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent introduces a transdermal delivery system comprising a cyclodextrin-based covalent organic framework and polymer as an intermediary carrier. This mediator facilitates active ingredient penetration through the stratum corneum barrier while maintaining skin protection, resolving the contradiction between barrier function and penetration efficiency

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The covalent organic framework employs a porous structure with controlled pore sizes to enable selective transport of active ingredients through the skin barrier. The porous material allows penetration of substances smaller than 100 to 200 nm while maintaining the barrier's protective function for larger molecules

Inventive Principle:

Principle #31Porous materials

2Productivity

If active ingredient size is reduced below 100 to 200 nm, then transdermal penetration is improved, but stability is worsened

Engineering Contradiction:

Improvetransdermal penetrationVSAvoidactive ingredient stability

Core Design Contradiction:

ProductivityVSStability of the object's composition

Solution Approach 1:

The patent employs a nested structure where the active ingredient is encapsulated within the cyclodextrin-based covalent organic framework, which is further integrated with a polymer matrix. This nested arrangement protects small active ingredients from degradation while maintaining their size for effective transdermal penetration

Inventive Principle:

Principle #7Nested doll (Nesting)

Solution Approach 2:

The transdermal delivery system uses a composite material comprising a cyclodextrin-based covalent organic framework combined with a polymer. This composite structure provides both the stability needed to protect small active ingredients and the penetration capability required for effective delivery

Inventive Principle:

Principle #40Composite materials

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 composite effectively transfers active ingredients into the skin in a stable form, demonstrating excellent efficacy even with small amounts over time, as shown by stability and particle size measurements.

Implementation Method 1

forming crystals in the crystallization solvent from the solution obtained in step (i) using a gas diffusion crystallizer

Methodology Applied

Scientific EffectGas diffusion: Diffusion

Implementation Method 2

forming crystals in the crystallization solvent from the solution obtained in step (i) using a gas diffusion crystallizer

Methodology Applied

Scientific EffectCrystallization: Crystallisation

Data Source

PatentUS12453692B2Transdermal delivery composite using covalent organic framework and polymer

Publication Date: 2025.10.28 H&A PHARMACHEM CO LTD

AI summary

The present invention relates to a transdermal delivery composite comprising a cyclodextrin-based covalent organic framework and polymer. In addition, the present invention relates to a cosmetic composition comprising the transdermal delivery composite, and a method for preparing the transdermal delivery composite.