Polyamine-dihydroxybenzoic acid hydrogel iron chelation

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Solution Overview

Problem

Current iron chelation therapies for managing iron overload, such as desferoxamine and deferiprone, have limitations including narrow therapeutic windows, systemic side effects, and toxicity issues, necessitating the development of a novel iron chelator with higher iron binding affinity and selectivity to safely remove excess iron from the body.

Innovation Solution

Development of polymeric chelators, specifically hydrogels formed by coupling polyamines with 2,3 dihydroxybenzoic acid, which exhibit high affinity and selectivity for iron, allowing for effective iron binding and removal from the gastrointestinal tract or bloodstream, reducing systemic side effects and toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If desferoxamine or deferiprone is used for iron chelation therapy, then iron binding occurs, but systemic side effects and toxicity increase

Engineering Contradiction:

Improveiron binding effectivenessVSAvoidsystemic side effects and toxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention divides the chelation therapy into localized action within the gastrointestinal tract using non-absorbable polymer chelators, separating the binding function from systemic circulation to eliminate systemic toxicity while maintaining local effectiveness

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent uses non-absorbable polymer chelators as intermediaries that bind iron in the GI tract and facilitate its excretion without entering systemic circulation, thereby mediating between iron overload and safe elimination without systemic side effects

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If desferoxamine is administered by subcutaneous infusion, then iron chelation occurs, but treatment complexity and patient burden increase due to 8-12 hours daily infusion requirement

Engineering Contradiction:

Improveiron chelation effectivenessVSAvoidadministration convenience

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The invention employs orally administered non-absorbable polymer chelators that act locally in the GI tract and are excreted, replacing the need for long-term infusion devices and reducing treatment to simple oral dosing

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent replaces the mechanical infusion system (subcutaneous pumps and tubing) with a chemical solution (oral polymer chelators) that achieves the same therapeutic effect through gastrointestinal action

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

3Reliability

If deferiprone or Exjade is administered orally, then iron binding occurs, but severe adverse effects such as neutropenia, agranulocytosis, and blood vessel inflammation occur

Engineering Contradiction:

Improveiron binding effectivenessVSAvoidsevere adverse effects including neutropenia and agranulocytosis

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention segments the chelation action to occur exclusively in the gastrointestinal tract using non-absorbable polymers, preventing the chelator from entering systemic circulation and causing blood-related adverse effects

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The non-absorbable polymer chelators serve as intermediaries that bind iron locally in the GI tract and promote excretion, mediating between iron overload and safe elimination without systemic absorption and associated toxicities

Inventive Principle:

Principle #24Intermediary (Mediator)

4Reliability

If current iron chelators are used, then iron removal occurs, but the therapeutic window is narrow making dose optimization difficult

Engineering Contradiction:

Improveiron removal effectivenessVSAvoidtherapeutic window flexibility

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention changes the key parameter of chelator absorption from systemic (current chelators) to localized GI tract action (polymer chelators), fundamentally altering the therapeutic profile to eliminate systemic toxicity while maintaining iron removal effectiveness

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 polymeric chelators demonstrate significantly higher iron binding affinity and selectivity compared to existing therapies, enabling rapid and safe removal of excess iron, potentially reducing the risk of adverse effects and improving treatment outcomes for iron overload conditions.

Implementation Method 1

Polyamine-dihydroxybenzoic acid conjugate hydrogels as iron chelators

Methodology Applied

Scientific EffectChelation: Adsorption

Data Source

PatentUS10039836B2Polyamine-dihydroxybenzoic acid conjugate hydrogels as iron chelators

Publication Date: 2018.08.07 UNIVERSITY OF KANSAS

AI summary

Compositions and methods for making a composition comprising a polymer and one or more chelators covalently coupled to polymer, wherein the one or more chelators has a benzene ring with more than one hydroxyl group at any position that is free, or a derivative of the chelator, or a salt of the chelator and methods of use.