Biodegradable Polyesteramide Copolymer Sustained Protein Release

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Solution Overview

Problem

Current drug delivery systems for proteins face challenges such as protein denaturing, burst release, incomplete release, and stability issues due to acidic byproducts from polymer degradation, limiting controlled and sustained release over an extended period.

Innovation Solution

A biodegradable polyesteramide copolymer composition with specific functional groups that absorbs water slowly, allowing for a sustained release of proteins over months to years, maintaining protein stability and activity through a controlled hydrolysis-driven biodegradation process.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hydrogel based drug delivery systems are used to solve incomplete release, then protein release completeness is improved, but release duration is limited to only a few weeks

Engineering Contradiction:

Improveprotein release completenessVSAvoidrelease duration

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent changes the physical and chemical parameters of the polymer matrix by using biodegradable polymers with controlled degradation rates. The polymer composition and molecular weight are optimized to maintain structural integrity for extended periods while enabling complete protein release through progressive degradation, thus achieving both complete release and extended duration

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material systems combining biodegradable polymers with specific functional groups and controlled crosslinking densities. This composite approach creates a matrix that balances mechanical stability for long-term durability with controlled porosity and degradation pathways for complete protein release over extended periods

Inventive Principle:

Principle #40Composite materials

2Duration of action of moving object

If biodegradable polymers like PLLA or PLGA are used for sustained release, then release duration is improved, but protein stability deteriorates due to acidic byproducts

Engineering Contradiction:

Improverelease durationVSAvoidprotein stability

Core Design Contradiction:

Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent converts the harmful acidic degradation byproducts into beneficial controlled-release mechanisms. The degradation products are designed to maintain a slightly acidic microenvironment that prevents protein aggregation while the bulk polymer matrix remains neutral, thus transforming a stability threat into a controlled release advantage

Inventive Principle:

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

Solution Approach 2:

The patent introduces intermediary buffering components and surface modification layers that mediate between the acidic degradation byproducts and the protein payload. These intermediaries neutralize harmful pH fluctuations while allowing sustained release, protecting protein stability without compromising release duration

Inventive Principle:

Principle #24Intermediary (Mediator)

3Speed

If rapid water absorption occurs in hydrogels, then protein release speed is improved, but release control is lost resulting in burst release

Engineering Contradiction:

Improveprotein release speedVSAvoidrelease control

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent creates a dynamic polymer matrix with time-dependent physical and chemical properties. The matrix transitions from an initial stable state with controlled permeability to a progressively degrading state, allowing the release speed to increase naturally over time while maintaining control through the structured degradation pathway, avoiding uncontrolled burst release

Inventive Principle:

Principle #15Dynamics

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 composition provides a uniform and sustained release of proteins over an extended period, reducing fluctuations and maintaining protein activity, while being compatible with the protein species, thus overcoming the limitations of existing hydrogel and polymer-based systems.

Implementation Method 1

a biodegradable polyesteramide copolymer composition with specific functional groups that absorbs water slowly, allowing for a sustained release of proteins over months to years, maintaining protein stability and activity through a controlled hydrolysis-driven biodegradation process

Methodology Applied

Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentEP2903592B1Drug delivery composition comprising proteins and biodegradable polyesteramides

Publication Date: 2019.01.23 DSM IP ASSETS BV

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AI summary

The present invention relates to a drug delivery composition comprising proteins and biodegradable polymers. The present invention further relates to a drug delivery system for controlled and long term release of proteins into a biological environment. The drug delivery composition comprises at least a protein and a biodegradable polymer possessing at least two different functional groups selected from the group of chosen among carboxyl-, ester-, amine-, amide-, thiol-, thioester- or hydroxyl groups pendant to the main polymer chain whereby the composition absorbs between 5-10% w/w water when exposed to physiological conditions for at least 20 days. The present invention further relates to a drug delivery system for controlled protein release comprising the composition. The drug delivery system may be chosen from microparticles, films, coatings, fibers, pellets, cylinders, discs, implants, microcapsules, microspheres, nanospheres, wafers, micelles, liposomes or woven or non-woven fabrics.