Transdermal Patch with Porator for Hydrophilic Drug Delivery

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Solution Overview

Problem

Conventional transdermal delivery systems face challenges in effectively delivering hydrophilic or large molecule drugs across the skin, as they struggle to achieve therapeutic levels due to limited permeability and flux, particularly for molecules larger than 1000 Daltons or those that are water-soluble.

Innovation Solution

A transdermal patch system that incorporates a polymer matrix with a hydrophilic permeant and a permeability enhancer, such as a pH control agent, which dissolves in biological moisture to facilitate the delivery of drugs like exenatide or insulin through the skin, utilizing a porator to create micropores for enhanced delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional transdermal delivery systems are used for hydrophilic or large molecule drugs, then the system structure is simple and easy to manufacture, but the transdermal flux and permeability are insufficient to achieve therapeutic levels

Engineering Contradiction:

Improvetransdermal fluxVSAvoidsystem complexity

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The system segments the delivery process into two distinct components: a porator device that creates micropores in the skin barrier, and a transdermal patch that delivers the hydrophilic permeant through the created pathways. This segmentation allows each component to be optimized independently - the porator for creating effective pathways and the patch for sustained permeant delivery - thereby achieving therapeutic flux levels without requiring a single complex integrated system.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The porator acts as an intermediary device that modifies the skin barrier to enable subsequent permeant delivery. By creating micropores in the stratum corneum, it mediates between the hydrophilic permeant (which cannot naturally penetrate the lipid-rich skin barrier) and the skin itself, allowing the simple patch structure to achieve high flux through the pre-created pathways.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If the permeant is hydrophilic and dissolves in biological moisture, then the permeant can be delivered through micropores, but the permeability through intact skin is insufficient

Engineering Contradiction:

Improvepermeant delivery reliabilityVSAvoidskin permeability barrier

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The porator performs preliminary action by creating micropores in the skin barrier before the permeant is applied. This pre-modification of the skin structure eliminates the permeability barrier for hydrophilic molecules, allowing them to dissolve in biological moisture and be reliably delivered through the pre-created pathways without encountering the intact skin's lipid barrier.

Inventive Principle:

Principle #10Preliminary action

3Quantity of substance

If micropores are created in the skin to enhance delivery, then the transdermal flux increases, but the duration of sustained delivery must be maintained

Engineering Contradiction:

Improvetransdermal fluxVSAvoidsustained delivery period

Core Design Contradiction:

Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

The patch design incorporates a polymer matrix with controlled permeant loading and composition that changes the release parameters over time. The matrix structure and permeant formulation are engineered to maintain a steady release rate through the micropores, ensuring both high flux and sustained delivery over the required treatment period.

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 system enables sustained delivery of hydrophilic permeants over extended periods, improving the transdermal flux and achieving therapeutic levels of drugs like exenatide and insulin, with enhanced permeability and bioavailability.

Implementation Method 1

the permeability enhancer is a pH control agent

Methodology Applied

Scientific EffectpH control:

Implementation Method 2

at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject

Methodology Applied

Scientific EffectDissolution: Solvation

Implementation Method 3

utilizing a porator to create micropores for enhanced delivery

Methodology Applied

Scientific EffectMicropore formation: Ablation

Implementation Method 4

The system enables sustained delivery of hydrophilic permeants over extended periods, improving the transdermal flux

Methodology Applied

Scientific EffectDiffusion: Diffusion

Data Source

PatentUS10493254B2Permeant delivery system and methods for use thereof

Publication Date: 2019.12.03 PASSPORT TECHNOLOGIES INC

AI summary

Disclosed are a patch, system, and method for delivery of a permeant composition into a subject via at least one formed pathway through a biological membrane of the subject. The patch comprises a matrix, at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the permeant can dissolve in biological moisture received from the subject, and at least one permeability enhancer disposed within the matrix. Also disclosed are systems and methods for delivery of a permeant composition into a subject via at least one formed pathway through a skin layer of the subject.