Polysaccharide Nanoparticle Preparation via Mild Oxidation

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current methods for preparing polysaccharide nanoparticles are complex and require harsh conditions, toxic chemicals, or surface-active compounds, making them unsuitable for therapeutic use due to toxicity and the need for extensive purification.

Innovation Solution

A process involving specific partial oxidation of polysaccharides to create aldehyde groups, followed by covalent bonding with hydrophobic nanoparticle-forming agents and therapeutic compounds in mild conditions, using oxidizing agents like periodate and pH-controlled reactions to form stable, biodegradable nanoparticles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional methods are used to prepare polysaccharide nanoparticles, then nanoparticles can be formed, but the process requires harsh conditions, toxic chemicals, and surface-active compounds

Engineering Contradiction:
Improvesuitability for therapeutic useVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters of the oxidation process by using mild oxidizing agents (periodate, bromine water) instead of harsh oxidants, and controls pH within physiological ranges (pH 2-9) to eliminate the need for toxic chemicals while maintaining nanoparticle formation capability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts and eliminates toxic components (surface-active compounds, aggressive chemicals) from the nanoparticle preparation process by using purely oxidative crosslinking of polysaccharides, which forms stable nanoparticles without requiring any toxic additives

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If conventional methods are used to prepare polysaccharide nanoparticles, then nanoparticles can be formed, but extensive purification is required

Engineering Contradiction:
Improvesuitability for therapeutic useVSAvoidpurification process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent removes the need for complex purification processes by eliminating toxic chemicals and surface-active compounds from the formulation, allowing direct use of the prepared nanoparticles for therapeutic applications without extensive cleaning steps

Inventive Principle:
Principle #2Taking out (Extraction)

3Stability of the object's composition

If oxidation degree is increased to improve nanoparticle stability, then nanoparticle stability improves, but toxicity increases

Engineering Contradiction:
Improvenanoparticle stabilityVSAvoidtoxicity
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the oxidation degree parameter within a specific range (0.1-80% of sugar rings) and uses mild oxidizing agents to achieve stable nanoparticles without generating toxic byproducts, resolving the contradiction between stability and toxicity

Inventive Principle:
Principle #35Parameter changes

4Reliability

If harsh conditions are used to prepare nanoparticles, then nanoparticle formation is achieved, but therapeutic compounds may be degraded

Engineering Contradiction:
Improvenanoparticle formationVSAvoidtherapeutic compound integrity
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the physical and chemical parameters of the preparation process by conducting oxidation at mild temperatures (0-100°C) and physiological pH levels, which preserves the integrity of sensitive therapeutic compounds while still achieving effective nanoparticle formation

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 process enables the production of non-toxic, biodegradable polysaccharide nanoparticles that can efficiently deliver therapeutic agents to targeted areas, such as tumors, with enhanced stability and reduced risk of drug resistance, while avoiding the use of aggressive chemicals and surfactants.

Implementation Method 1

specific partial oxidation of polysaccharides to create aldehyde groups

Methodology Applied
Scientific EffectOxidation: Oxidation

Implementation Method 2

using oxidizing agents like periodate

Methodology Applied
Scientific EffectPeriodate oxidation:

Implementation Method 3

covalent bonding with hydrophobic nanoparticle-forming agents and therapeutic compounds

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Implementation Method 4

coupling reaction between a terminal aldehyde group of the modified polysaccharide and a functional group of the protein able to react with said aldehyde group

Methodology Applied
Scientific EffectSchiff base formation:

Implementation Method 5

attaching hydrophobic compounds, including medicaments

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Data Source

PatentEP2825563B1Process for the preparation of polysaccharide nanoparticles
Publication Date: 2020.02.05 NANOVELOS
  • EP2825563B1 patent drawingFigure 1~2

AI summary

The process for the preparation of nanoparticles from polysaccharides and derivatives thereof, by their specific partial oxidation to produce aldehyde groups and attach compounds with amino or other group with the R-NH2 bond which react with aldehyde groups, comprising oxidizing the polysaccharide or derivative thereof by a known method to obtain aldehyde groups until the oxidation degree of 0,1% to 80% of the sugar rings is obtained, then adding at least one nanoparticle-forming agent which after attachment of the aldehyde group exhibits hydrophobic properties, selected from the group comprising: aliphatic or aromatic organic amines containing from 4 to 20 carbon atoms, amides and hydrazides of aliphatic and aromatic organic acids containing from 4 to 20 carbon atoms, hydrophobic amino acids, phosphatidylethanolamine, and at least one active substance containing at least one amino, amido or hydrazide group, to the solution of the oxidized polysaccharide in water or a mixture of water and an organic solvent, carrying the reaction out at pH of the solution from 1 to 9, at the temperature of from 10 to 100°C, wherein the total molar ratio of amino groups to aldehyde groups is from 20 to 0,5.