Gallate Matrix Solubilizes Water-Insoluble Therapeutics

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Solution Overview

Problem

Current medical devices face challenges in effectively delivering water-insoluble therapeutic agents to specific sites within the body due to their insolubility in aqueous environments, leading to inadequate treatment of conditions like restenosis after procedures like PTCA, where the therapeutic agents may not be optimally released at the intended site.

Innovation Solution

Incorporating a water-insoluble therapeutic agent into a matrix of a gallate-containing compound, such as epi gallate catechin gallate (EGCG) or tannic acid, which enhances the solubility and delivery of the agent to the vessel wall and tissue, allowing for localized treatment without additional polymer or non-polymer carriers that modify the release rate.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a water-insoluble therapeutic agent is used in a coating, then the coating can be durable during delivery, but the therapeutic agent cannot be optimally delivered at the target site due to insolubility in aqueous environments

Engineering Contradiction:
Improvecoating durabilityVSAvoidtherapeutic agent delivery
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent introduces gallate-containing compounds as intermediary substances that mediate between the water-insoluble therapeutic agent and the aqueous biological environment. These compounds form a matrix that solubilizes the therapeutic agent, enabling it to be delivered effectively while maintaining coating durability during delivery

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the solubility parameter of the therapeutic agent by incorporating it into a matrix of gallate-containing compounds. This transformation allows the otherwise water-insoluble agent to become soluble in aqueous environments, enabling effective delivery without compromising coating integrity

Inventive Principle:
Principle #35Parameter changes

2Reliability

If additional polymer or non-polymer carriers are used to enhance therapeutic agent delivery, then solubility is improved, but device complexity increases

Engineering Contradiction:
Improvetherapeutic agent solubilityVSAvoidcoating composition
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The gallate-containing compound serves multiple functions simultaneously: it acts as a solubilizing agent, forms a durable coating matrix, and provides structural integrity. This multi-functionality eliminates the need for separate carrier polymers or non-polymer additives, simplifying the overall coating composition while maintaining effective therapeutic agent delivery

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 gallate-containing compounds significantly increases the solubility and delivery of water-insoluble therapeutic agents, ensuring a therapeutically effective amount is reached at the treatment site, thereby improving treatment outcomes for conditions like restenosis.

Implementation Method 1

the gallate containing compound increases the solubility of the water-insoluble therapeutic agent in an aqueous medium

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 2

enhances the delivery of the water-insoluble therapeutic agent to a vessel wall and into the tissue of a patient

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS20240245839A1Compositions and devices incorporating water-insoluble therapeutic agents and methods of the use thereof
Publication Date: 2024.07.25 COOK MEDICAL TECHNOLOGIES LLC
  • US20240245839A1 patent drawing
  • US20240245839A1 patent drawing
  • US20240245839A1 patent drawing

AI summary

Various aspects of the present invention provide compositions and implantable devices including a water-insoluble therapeutic agent solubilized in a matrix of a gallate-containing compound. Other aspects provide methods of manufacturing and using such compositions and devices.