Mercapto-Modified Biocompatible Macromolecules for Low-Crosslinking

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Solution Overview

Problem

Current biocompatible macromolecules used in medical applications have a high degree of modification or cross-linking, which alters their physiological function and biocompatibility, leading to side effects and reduced effectiveness, while a low degree of modification or cross-linking results in short in vivo duration and high solubility, limiting their clinical applications.

Innovation Solution

Development of mercapto-modified biocompatible macromolecule derivatives with a low degree of mercapto-modification and disulfide-bond cross-linked biocompatible macromolecule materials, allowing for effective chemical cross-linking that maintains initial structure and function while reducing solubility and improving in vivo duration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If biocompatible macromolecules are highly chemically modified or cross-linked, then their in vivo duration is prolonged and solubility is reduced, but their physiological function and biocompatibility are altered and side effects occur

Engineering Contradiction:
Improvein vivo durationVSAvoidside effects
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by precisely controlling the degree of mercapto-modification to be low (≤4.5%), which is a specific quantitative parameter. This low degree of modification allows the macromolecule to maintain its physiological function and biocompatibility while still achieving the desired effect of prolonged in vivo duration and reduced solubility through disulfide bond cross-linking. The parameter change resolves the contradiction by finding an optimal low threshold that satisfies both requirements.

Inventive Principle:
Principle #35Parameter changes

2Loss of substance

If biocompatible macromolecules are chemically modified or cross-linked, then their solubility in vivo is reduced, but their physiological function and biocompatible property are reduced

Engineering Contradiction:
Improvesolubility reductionVSAvoidphysiological function
Core Design Contradiction:
Loss of substanceVSReliability

Solution Approach 1:

The patent changes the parameter of modification degree to a low level (≤4.5%) and uses disulfide bond cross-linking instead of traditional high-degree chemical modification. This parameter change enables the macromolecule to reduce solubility in vivo through cross-linking while maintaining physiological function because the low degree of mercapto-modification preserves the original macromolecule structure and properties.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces disulfide bonds as an intermediary mechanism to achieve solubility reduction without direct high-degree chemical modification of the macromolecule. The disulfide bonds form cross-links between macromolecule chains, reducing solubility, while the low degree of mercapto-modification ensures that the macromolecule's physiological function remains intact. The disulfide bond acts as a mediator that achieves the desired effect without directly altering the macromolecule's functional groups.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If biocompatible macromolecules are highly cross-linked, then their stability is improved, but their initial structure is altered

Engineering Contradiction:
ImprovestabilityVSAvoidinitial structure
Core Design Contradiction:
Stability of the object's compositionVSShape

Solution Approach 1:

The patent changes the parameter of cross-linking degree to a low level, achieved through low degree of mercapto-modification (≤4.5%). This parameter change allows the formation of disulfide bond cross-links that provide stability without requiring high degrees of modification. The low cross-linking degree preserves the initial structure of the macromolecule while still achieving improved stability through the formation of cross-linked networks.

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 low degree of modification and cross-linking enhances biocompatibility, stability, and clinical applicability, providing a sustained release carrier and effective treatment for osteoarthritis and wound healing with reduced side effects and improved shelf-life.

Implementation Method 1

disulfide-bond cross-linked biocompatible macromolecule materials

Methodology Applied
Scientific EffectDisulfide bond formation: Oxidation

Data Source

PatentUS10064889B2Mercapto-modified biocompatible macromolecule derivatives with low degree of mercapto-modification and the cross-linked materials and uses thereof
Publication Date: 2018.09.04 BIOREGEN BIOMEDICAL (CHANGZHOU) CO LTD
  • US10064889B2 patent drawing

AI summary

The present invention discloses a mercapto-modified biocompatible macromolecule derivative with a low degree of modification. The mercapto-modified biocompatible macromolecule derivative not only maintains the initial structure, physiological function and biocompatibility as much as possible, but also allows the preparation of the biocompatible macromolecule cross-linked material with a low degree of cross-linking through the effectively chemical cross-linking with the introduced mercapto group. The present invention further discloses a disulfide-bond cross-linked biocompatible macromolecule material with a very low degree of cross-linking. The disulfide-bond cross-linked biocompatible macromolecule material not only maintains the initial structure, physiological function and biocompatibility of the biocompatible macromolecule as much as possible, but also effectively prolongs turn over and reduces the solubility of the biocompatible macromolecule in vivo, better meeting the requirements of various clinical applications. The present invention further relates to the application of the disulfide-bond cross-linked biocompatible macromolecule material in the field of medicine and pharmacy.