Vacant Vesicle Encapsulation via Segmented Self-Assembly

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Solution Overview

Problem

Current methods for producing substance-encapsulating vesicles through self-assembly of polymers face challenges such as interference of the encapsulation-target substance with vesicle formation, use of organic solvents damaging the substance, and difficulty in achieving uniform particle size and structure, making them inefficient and impractical for various applications.

Innovation Solution

A method involving the mixing of a vacant vesicle with an encapsulation-target substance in an aqueous medium, utilizing block copolymers with uncharged hydrophilic and charged segments to form vesicles that encapsulate substances like proteins, polypeptides, and nucleic acids without disrupting the vesicle structure, allowing for efficient and uniform encapsulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If the simultaneous mixing method is used to produce substance-encapsulating vesicles, then the vesicle formation and substance encapsulation occur in one step, but the encapsulation-target substance interferes with vesicle formation and organic solvents damage the substance

Engineering Contradiction:
Improveproduction efficiencyVSAvoidvesicle formation stability
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The process is divided into two separate steps: first forming vacant vesicles using block copolymers in an aqueous medium, then introducing the encapsulation-target substance into the vesicle cavity. This segmentation prevents the substance from interfering with vesicle formation while avoiding organic solvent damage.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The vacant vesicles are prepared in advance before introducing the encapsulation-target substance. This preliminary formation of the vesicle structure allows the substance to be encapsulated without affecting the self-assembly process, and eliminates the need for organic solvents during vesicle formation.

Inventive Principle:
Principle #10Preliminary action

2Productivity

If the simultaneous mixing method is used, then encapsulation occurs during vesicle formation, but uniform particle size and structure cannot be achieved

Engineering Contradiction:
Improveproduction efficiencyVSAvoidparticle size uniformity
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

Separating vesicle formation from substance encapsulation allows each process to be optimized independently. The vesicle formation step produces uniform vacant vesicles through controlled self-assembly, while the subsequent substance introduction maintains this uniformity without interference.

Inventive Principle:
Principle #1Segmentation

3Ease of manufacture

If organic solvents are used in the simultaneous mixing method, then vesicle formation is facilitated, but the encapsulation-target substance is damaged

Engineering Contradiction:
Improvevesicle formation easeVSAvoidsubstance damage
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The invention changes the solvent parameter from organic to aqueous medium for vesicle formation. Block copolymers with hydrophilic segments enable spontaneous vesicle formation in water without requiring organic solvents, thereby preventing damage to the encapsulation-target substance while maintaining ease of manufacture.

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

This method enables the easy and efficient production of substance-encapsulating vesicles with high stability and controllability, suitable for drug delivery systems and other applications, by maintaining the vesicle structure and allowing for the encapsulation of multiple active ingredients.

Implementation Method 1

a vesicle can be formed via self-assembly of polymers of which the primary structures have been controlled precisely

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

an electrostatically-united polymeric micelle formed via self-assembly of a block copolymer having an uncharged segment and a charged segment

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Data Source

PatentEP3417934B1Substance-encapsulating vesicle and process for producing the same
Publication Date: 2023.12.27 THE JAPAN SCI & TECH AGENCY
  • EP3417934B1 patent drawingFigure 1~1(b)
  • EP3417934B1 patent drawingFigure 2~3(b)
  • EP3417934B1 patent drawingFigure 4~4(b)

AI summary

Provided is a method for easily and efficiently producing encapsulated substance vesicles wherein a substance is encapsulated in the cavity of vesicles obtained by polymer self-assembly. Empty vesicles that have membranes comprising a first polymer that is a block copolymer with uncharged hydrophilic segments and a first kind of charged segments and a second polymer with a second kind of charged segments that carry a charge that is the opposite of said first kind of charged segments as well as spaces that are enclosed by said membranes are mixed in an aqueous medium with the substance that is to be encapsulated in the spaces.