Extracellular Matrix Compositions for Transdermal Delivery

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Solution Overview

Problem

Current transdermal and transmucosal delivery systems face challenges with toxic penetration enhancers, skin irritation, and inability to deliver high molecular weight pharmaceuticals and cosmetic agents effectively, necessitating a safe and efficient method for administering a wide range of active agents through the skin and mucosa.

Innovation Solution

Compositions containing active agents and extracellular matrix components or fragments, such as hyaluronic acid, collagen, and elastin, which disrupt cell-cell and cell-scaffold attachments to enhance penetration, allowing for the delivery of various pharmaceuticals and cosmetic agents through the skin and mucosa.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If traditional penetration enhancers are used to enhance transdermal absorption, then penetration efficiency is improved, but skin irritation and toxicity occur

Engineering Contradiction:
Improvetransdermal absorption efficiencyVSAvoidskin irritation and toxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses extracellular matrix components (collagen, elastin, fibronectin, laminin) as intermediary substances that facilitate transdermal absorption without causing skin irritation or toxicity. These natural components act as mediators between the drug and skin, providing a safe pathway for penetration enhancement while maintaining skin integrity and biocompatibility.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical and physical parameters of the penetration enhancer by using naturally occurring extracellular matrix components with specific molecular weights (2,000-60,000 daltons) instead of traditional synthetic enhancers. This parameter change maintains penetration efficiency while eliminating the harmful effects associated with conventional penetration enhancers.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If conventional delivery systems are used, then simple molecules can be delivered, but high molecular weight pharmaceuticals and cosmetic agents cannot be delivered effectively

Engineering Contradiction:
Improvemolecular weight of deliverable agentsVSAvoiddelivery effectiveness
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The extracellular matrix components serve as intermediaries that can accommodate and transport high molecular weight substances through the skin. These natural polymers create a pathway that is compatible with large molecules, allowing them to penetrate the skin barrier effectively without degradation or loss of therapeutic activity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs composite formulations combining extracellular matrix components with high molecular weight pharmaceuticals and cosmetic agents. This composite approach creates a synergistic system where the natural polymer matrix facilitates the delivery of large molecules that would otherwise be unable to penetrate the skin effectively.

Inventive Principle:
Principle #40Composite materials

3Productivity

If topical compositions are applied to enhance penetration, then absorption is improved, but skin thinning occurs with prolonged use

Engineering Contradiction:
Improvepenetration enhancementVSAvoidskin thickness and integrity
Core Design Contradiction:
ProductivityVSStrength

Solution Approach 1:

The patent converts the potential harm of prolonged penetration enhancement into a benefit by using extracellular matrix components that not only enhance absorption but also support skin structure and health. These natural components can be used continuously without causing skin thinning, as they work with rather than against the skin's natural architecture.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent changes the nature of the penetration enhancer from aggressive synthetic chemicals to gentle natural extracellular matrix components. This parameter change allows for prolonged use without the adverse effect of skin thinning, as the natural components maintain skin integrity while facilitating ongoing drug delivery.

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 use of extracellular matrix components as decoy molecules in topical compositions significantly enhances the delivery of active agents, achieving deeper penetration and improved bioavailability, while minimizing skin irritation and toxicity, thus providing a safe and effective transdermal delivery system.

Implementation Method 1

decoy molecules that are capable of causing rearrangement of tissues that the composition contacts by temporarily disrupting cell-cell (i.e. intercellular) and cell-scaffold attachment

Methodology Applied
Scientific EffectCell-cell attachment disruption:

Data Source

PatentUS20190008795A1Compositions for topical application of compounds
Publication Date: 2019.01.10 ILLUSTRIS PHARMACEUTICALS INC
  • US20190008795A1 patent drawing
  • US20190008795A1 patent drawing
  • US20190008795A1 patent drawing

AI summary

Compositions for transdermal delivery of an active agent and methods for using such compositions are described herein.