Solid-Forming Local Anesthetic Formulation for Neuropathic Pain

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Solution Overview

Problem

Current treatments for neuropathic pain, such as postherpetic neuralgia and diabetic neuropathies, often require rapid-acting and long-lasting solutions that existing formulations fail to provide effectively, with a need for improved delivery methods that enhance adherence to the skin and maintain therapeutic efficacy.

Innovation Solution

A solid-forming local anesthetic formulation comprising a local anesthetic, water, and a polymer, which forms a coherent soft solid upon evaporation of water, allowing direct application to the skin without a backing layer, enhancing adherence and prolonged delivery of the anesthetic for pain relief.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If traditional liquid or cream formulations are used for neuropathic pain treatment, then the formulation can be easily applied to the skin, but the formulation fails to provide sufficient adherence to the skin and prolonged delivery of the anesthetic

Engineering Contradiction:
Improveduration of analgesic effectVSAvoidadherence to skin
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The formulation utilizes phase transition of water from liquid to vapor through evaporation, transforming the formulation from a liquid/cream state to a solidified state that adheres to the skin. This phase change enables the formulation to provide both ease of application (when liquid) and prolonged adherence (when solidified), resolving the contradiction between applicability and skin retention.

Inventive Principle:
Principle #36Phase transitions

Solution Approach 2:

The formulation changes its physical parameters (viscosity, state of matter) over time through controlled evaporation of water. Initially, the formulation has low viscosity for easy application, then progressively increases in viscosity and eventually solidifies to provide sustained adherence and drug delivery, thereby achieving both ease of application and prolonged duration of action.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If a backing layer or support substrate is used in traditional transdermal patches, then the formulation can be applied to the skin, but the formulation cannot adhere to skin regions that do not readily lend themselves to traditional patches

Engineering Contradiction:
Improveadherence to difficult skin regionsVSAvoidstructure of formulation system
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention extracts and eliminates the backing layer or support substrate from the traditional transdermal patch system. By removing this component, the formulation can directly contact and adhere to the skin surface, including irregular or difficult-to-reach areas, while maintaining structural integrity through self-solidification upon water evaporation.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The formulation serves its own structural support function through self-solidification. Instead of relying on an external backing layer for structural support, the formulation itself transforms into a solid state that provides both structural integrity and skin adherence, eliminating the need for separate support components.

Inventive Principle:
Principle #25Self-service

3Duration of action of moving object

If existing formulations are used for neuropathic pain, then treatment can be provided, but the formulations fail to provide rapid-acting and long-lasting relief simultaneously

Engineering Contradiction:
Improveduration of pain reliefVSAvoidonset of pain relief
Core Design Contradiction:
Duration of action of moving objectVSSpeed

Solution Approach 1:

The formulation provides continuous delivery of the local anesthetic through controlled evaporation of water. As water evaporates progressively, the anesthetic is continuously released and delivered to the skin and underlying tissues, ensuring both rapid initial effect (when formulation is first applied) and sustained long-lasting relief (as evaporation continues over time).

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The formulation utilizes periodic evaporation of water molecules from the surface, creating a sustained release mechanism. This periodic loss of water molecules drives continuous progression from liquid to solid state, maintaining continuous anesthetic delivery over an extended period while providing both rapid onset and prolonged duration.

Inventive Principle:
Principle #19Periodic 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

The formulation provides significant pain relief within 45 minutes, with sustained analgesic effects lasting up to 6 hours, as demonstrated in clinical trials, offering a more effective and longer-lasting treatment for neuropathic pain compared to traditional methods.

Implementation Method 1

the formulation layer to solidify into a coherent soft solid as water evaporates from the formulation layer

Methodology Applied
Scientific EffectEvaporation: Evaporation

Data Source

PatentEP2378873B1Method of treating neuropathic pain
Publication Date: 2017.08.23 CRESCITA THERAPEUTICS INC
  • EP2378873B1 patent drawingFigure 1
  • EP2378873B1 patent drawingFigure 2

AI summary

A method for treating subjects experiencing neuropathic pain is provided. The method involves the application of a solid-forming local anesthetic formulation to a skin surface of the subject experiencing the neuropathic pain and then maintaining the formulation on the skin surface for a period of time sufficient to allow itself to transdermally deliver the local anesthetic to the subject thereby providing relief from the neuropathic pain within about 45 minutes.