Polyamine Iontophoretic Composition for Cationic Drug Delivery

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Solution Overview

Problem

Current transdermal delivery methods, particularly iontophoresis, face inefficiencies in delivering cationic active agents due to depletion of electrolytes, leading to fluctuations in electrical field strength and potential skin irritation, and are inadequate for rapid onset of action and high-dose administration.

Innovation Solution

Incorporation of polyamines or polyamine salts into an iontophoretic reservoir composition, forming an aqueous or gelled skin-contacting composition that enhances iontophoretic transdermal delivery by maintaining electrical field strength and reducing skin irritation, allowing for higher current intensities without significant adverse effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional iontophoretic delivery is used with background electrolytes, then iontophoretic transdermal delivery can be achieved, but the electrical field strength fluctuates and skin irritation occurs

Engineering Contradiction:

Improveelectrical field strength consistencyVSAvoidskin irritation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent removes background electrolytes from the iontophoretic composition formulation. By eliminating NaCl and other background electrolytes that traditionally accompany cationic active agents, the invention prevents electrolyte depletion during iontophoresis, thereby maintaining consistent electrical field strength and avoiding skin irritation caused by electrolyte accumulation.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs a composite gel formulation consisting of carbomer (polyacrylic acid) and triethanolamine in a specific ratio (95:5 to 5:95 weight percent). This composite material system provides both the necessary ionic conductivity for iontophoresis and buffering capacity to maintain pH stability, while avoiding the harmful effects of traditional background electrolytes.

Inventive Principle:

Principle #40Composite materials

2Productivity

If higher current intensities are applied for high-dose administration, then delivery efficiency improves, but skin irritation increases

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidskin irritation

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent converts the traditionally harmful effect of background electrolytes into a beneficial absence. By formulating without background electrolytes, the invention allows higher current intensities to be applied safely, as there are no electrolytes to deplete or accumulate and cause irritation. This enables high-dose administration with improved delivery efficiency while maintaining skin tolerance.

Inventive Principle:

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

3Speed

If rapid onset of action is achieved through iontophoresis, then delivery speed improves, but electrolyte depletion occurs causing field strength fluctuations

Engineering Contradiction:

Improvedelivery speedVSAvoidelectrical field strength

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent extracts and eliminates background electrolytes from the formulation. This removal prevents the electrolyte depletion phenomenon that occurs during rapid iontophoretic delivery, ensuring that electrical field strength remains stable and predictable even at high delivery speeds, thereby enabling rapid onset of action without field strength fluctuations.

Inventive Principle:

Principle #2Taking out (Extraction)

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 polyamine-containing compositions enable efficient, rapid, and safe transdermal iontophoretic delivery of cationic active agents, maintaining consistent delivery and avoiding skin irritation, even at higher current intensities, thus overcoming the limitations of existing methods.

Implementation Method 1

iontophoretic transdermal delivery of cationic active agents

Methodology Applied

Scientific EffectIontophoresis: Iontophoresis

Implementation Method 2

maintaining electrical field strength

Methodology Applied

Scientific EffectElectrical field: Electric Field

Implementation Method 3

reducing skin irritation, allowing for higher current intensities without significant adverse effects

Methodology Applied

Scientific EffectIontophoresis: Iontophoresis

Data Source

PatentUS10881607B2Composition for transdermal delivery of cationic active agents

Publication Date: 2021.01.05 LTS LOHMANN THERAPIE SYST AG

AI summary

The invention relates to a composition for transdermal delivery, particularly iontophoretic transdermal delivery, of at least one cationic active agent or a salt thereof. The composition includes at least one cationic active agent or a salt thereof, at least one polyamine or/and polyamine salt, water or an aqueous solvent mixture, and optionally one or more additives. The invention further relates to the use of such composition as a component of a transdermal patch or of an iontophoretic transdermal patch, as well as to the use of such composition in a method for transdermally and/or iontophoretically administering cationic active agents. The invention further includes methods for determining the in vitro skin permeation properties of an active-agent-containing iontophoretic composition.