Covalent Drug-Polymer Copolymers for Uniform Coating Release

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Solution Overview

Problem

Current drug release systems for medical devices face challenges such as impurities triggering adverse biological responses, phase separation compromising mechanical properties, and instability of biologically active agents, leading to non-uniform distribution and reduced efficacy.

Innovation Solution

Development of compounds with biologically active agents linked via oligomeric segments, forming a stable coating that ensures uniform distribution and controlled release of drugs, maintaining mechanical properties and stability, using structures like Bio-Link-Bio-R, where Bio units are anti-inflammatory agents and Link is an oligomeric organic, organosilicon, or organosulfone segment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If biologically active agents are mixed with polymer platform in solvent system, then drug delivery is achieved, but phase separation occurs compromising mechanical properties

Engineering Contradiction:
Improvedrug delivery effectivenessVSAvoidmechanical properties of coating
Core Design Contradiction:
ReliabilityVSStrength

Solution Approach 1:

The patent combines the biologically active agent and polymer platform into a single copolymer structure where the drug is incorporated into the polymer backbone or side chains. This merging eliminates phase separation by ensuring molecular-level mixing, while the copolymer maintains mechanical integrity through its unified polymeric structure.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite copolymer material where hydrophilic drug-containing segments and hydrophobic polymer segments are covalently bonded. This composite structure at the molecular level prevents macroscopic phase separation while maintaining the mechanical properties needed for coating applications.

Inventive Principle:
Principle #40Composite materials

2Duration of action of stationary object

If biologically active agents are incorporated into polymer, then extended release is achieved, but impurities trigger adverse biological responses

Engineering Contradiction:
Improvedrug release durationVSAvoidadverse biological responses
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of the biologically active agent by incorporating it into the polymer chain, changing its physical state from free drug to polymer-bound drug. This parameter change allows controlled release through polymer degradation or dissolution, extending duration while the pure copolymer structure eliminates impurity-related adverse responses.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If biologically active agents are mixed with polymer, then drug release is achieved, but uniform distribution is compromised

Engineering Contradiction:
Improvedrug release functionalityVSAvoiduniform distribution of drug
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

By merging the drug molecule with the polymer chain through covalent bonding during copolymerization, the patent achieves uniform distribution at the molecular level. Each polymer chain contains drug units distributed throughout its structure, ensuring homogeneous drug placement without the aggregation problems of simple mixing.

Inventive Principle:
Principle #5Merging (Combining)

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 solution provides a stable and uniform drug release profile, maintaining mechanical properties and ensuring localized therapeutic concentrations, with reduced biological activity, enhancing the compatibility and effectiveness of the drug delivery system.

Implementation Method 1

compounds with biologically active agents linked via oligomeric segments

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Implementation Method 2

The biologically active agent is then released by particle dissolution or diffusion

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 3

it may be released as the polymer enzymatically degrades or disintegrates in the body

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentEP3357522B1Coated medical article for drug release
Publication Date: 2019.10.16 RIPPLE THERAPEUTICS CORP
  • EP3357522B1 patent drawingFigure 1-A
  • EP3357522B1 patent drawingFigure 1-B
  • EP3357522B1 patent drawingFigure 2A~2D

AI summary

The invention relates to compounds that include biologically active agents (e.g., compounds according to any of formulas (I) and (I-A) that can be used for effective drug release, e.g., as coatings for medical devices. Use of these compounds in the coating of surfaces can allow for long-term drug release as well as imparting uniform coatings with little phase separation compared to, e.g., the parent biologically active agent.