Block Copolymers for Drug Delivery via Hydrolysable Linkages

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Solution Overview

Problem

Current amphiphilic block copolymers used in pharmaceutical agent delivery face challenges in forming stable supramolecular structures in aqueous environments, particularly in introducing biological molecules and achieving asymmetric block copolymers under anhydrous conditions, limiting their effectiveness in pharmacological applications.

Innovation Solution

Development of block copolymers with hydrophilic and hydrophobic blocks interrupted by hydrolysable or oxidation-sensitive chemical moieties, such as esters, amides, or thioesters, that self-assemble into micelles or vesicles, allowing for efficient encapsulation and delivery of pharmaceutical agents like nucleic acids and drugs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If block copolymers are prepared via ionic polymerization under strictly anhydrous conditions, then the polymerization process is stable and controllable, but it becomes difficult to obtain asymmetric block copolymers or to introduce biological molecules

Engineering Contradiction:
Improvepolymerization process stabilityVSAvoidability to introduce biological molecules
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the polymerization conditions from strictly anhydrous to aqueous or humid conditions, allowing the incorporation of hydrophilic blocks and biological molecules while maintaining controlled polymerization through modified ionic polymerization mechanisms

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses water or aqueous solutions as an intermediary medium to enable the incorporation of hydrophilic blocks and biological molecules during polymerization, while maintaining control through controlled water content and pH conditions

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If block copolymers are designed with hydrophilic and hydrophobic blocks for self-assembly, then supramolecular structures like micelles and vesicles can be formed, but the stability of these structures in aqueous environments is challenging

Engineering Contradiction:
Improveself-assembly capabilityVSAvoidsupramolecular structure stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent introduces locally modified blocks with specific hydrophilic or hydrophobic properties, including charged blocks and oxidation-sensitive moieties, to create localized regions that enhance self-assembly and stabilize supramolecular structures in aqueous environments

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent creates composite block copolymer structures combining different polymer blocks with specific functional groups (hydrophilic blocks, hydrophobic blocks, charged blocks, oxidation-sensitive moieties) to achieve both self-assembly capability and environmental stability

Inventive Principle:
Principle #40Composite materials

3Ease of manufacture

If block copolymers are made biodegradable with hydrolysable groups, then they can be cleared from the body, but the degradation rate and encapsulation efficiency need to be controlled

Engineering Contradiction:
ImprovebiodegradabilityVSAvoiddegradation rate control
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent modifies the hydrolysable groups and block copolymer composition to control degradation rate, using parameters such as pH, temperature, and specific chemical moieties (esters, amides, thioesters, anhydrides, ketals) to achieve controlled biodegradation and encapsulation efficiency

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2356228B1Block copolymers and uses thereof
Publication Date: 2023.05.03 ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
  • EP2356228B1 patent drawingFigure 1A
  • EP2356228B1 patent drawingFigure 1B
  • EP2356228B1 patent drawingFigure 1C

AI summary

An encoding/decoding apparatus and method using a low-density parity-check code (LDPC code) is disclosed. Basic column group information, serving as a set of information regarding positions of rows with weight 1, is extracted from a reference column in each column group of a predetermined parity-check matrix. Column group information transforms the positions of rows with weight 1 into positions whose lengths are within a required parity length. A parity-check matrix is generated according to the generated column group information. Data is encoded or decoded based on the generated parity-check matrix.