Treprostinil Transdermal Patches for Sustained, Low-Irritation Delivery

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Solution Overview

Problem

Current treatments for pulmonary hypertension, such as treprostinil, face challenges with oral bioavailability, short half-life, and discomfort from subcutaneous or intravenous administration, and inhalation methods cause lung irritation and plasma concentration peaks.

Innovation Solution

Dermal and transdermal administration of treprostinil and its salts using patches with chemical or physical enhancement techniques to enhance skin permeability, including iontophoresis, microneedles, and chemical permeation enhancers, allowing for passive or active transport.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If subcutaneous or intravenous injection is used to administer treprostinil, then the drug can be effectively delivered to treat PH, but it causes pain at the site of injection and risk of infection

Engineering Contradiction:

Improvedrug delivery effectivenessVSAvoidpain and infection risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the mechanical injection system (needles, syringes) with a transdermal patch system that delivers drug through the skin barrier without puncturing the body, eliminating injection-site pain and infection risk while maintaining effective drug delivery

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent introduces permeation enhancers as intermediary substances that facilitate drug transport through the skin barrier, allowing the drug to penetrate the stratum corneum and reach target tissues without requiring invasive injection methods

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If oral administration is used, then it is convenient for patients, but treprostinil has absolute oral bioavailability of less than 10% due to significant metabolism

Engineering Contradiction:

Improvepatient convenienceVSAvoidbioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent extracts the drug from the gastrointestinal tract and hepatic metabolism system by delivering it directly through the skin, bypassing the first-pass metabolism that causes <10% bioavailability while maintaining patient convenience

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses permeation enhancers as intermediaries to facilitate skin penetration, allowing the drug to enter the systemic circulation through the skin barrier rather than through the gastrointestinal tract, thereby avoiding metabolic degradation

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If inhalation is used to administer treprostinil, then it can be delivered to the lungs, but about 50% of PAH patients cannot take it due to irritation to the lungs

Engineering Contradiction:

Improvedrug delivery to lungsVSAvoidlung irritation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the inhalation system with a transdermal delivery system, eliminating the need for patients to inhale the drug and thereby avoiding lung irritation while still achieving effective systemic delivery for treating PH

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

4Reliability

If inhalation is used, then treprostinil can be administered, but it exhibits a large peak-to-trough ratio of plasma concentrations

Engineering Contradiction:

Improvedrug administrationVSAvoidplasma concentration stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent implements continuous drug release through the transdermal patch, maintaining stable plasma concentrations over time by providing sustained delivery without the large peak-to-trough fluctuations associated with inhalation, thereby improving concentration stability

Inventive Principle:

Principle #20Continuity of useful action

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

Provides increased local or systemic availability of treprostinil without significant skin irritation, offering controlled, continuous, and sustained release, reducing discomfort and improving patient compliance.

Implementation Method 1

passive transport of treprostinil as the carboxylic acid in some embodiments, optionally with the use of one or more chemical permeation enhancers

Methodology Applied

Scientific EffectPermeation: Permeation

Implementation Method 2

actively with the assistance of a physical enhancement technique (e.g., an iontophoretic patch)

Methodology Applied

Scientific EffectIontophoresis: Iontophoresis

Implementation Method 3

physical enhancement technique (e.g., an iontophoretic patch, a sonophoretic patch, a microneedles patch)

Methodology Applied

Scientific EffectMechanical disruption: Abrasion

Implementation Method 4

physical enhancement technique (e.g., an iontophoretic patch, a sonophoretic patch)

Methodology Applied

Scientific EffectAcoustic cavitation: Acoustic Cavitation

Data Source

PatentUS20250205173A1Dermal and transdermal administration of treprostinil and salts thereof

Publication Date: 2025.06.26 CORSAIR PHARMA INC

AI summary

The present disclosure provides methods, compositions, devices and systems for dermal and transdermal administration of treprostinil or salts thereof, and optionally an additional therapeutic agent. Treprostinil and salts thereof can be dermally or transdermally administered to treat any medical conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.