Amphiphilic Block Copolymer Particles for Drug Delivery

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Solution Overview

Problem

Current block copolymers and microparticles/nanoparticles lack effective methods for forming amphiphilic structures that can selectively solubilize and deliver biologically active agents across biological barriers, such as the blood-brain barrier, and efficiently remove undesirable substances from fluids.

Innovation Solution

Development of amphiphilic linear block copolymers synthesized from polysaccharides and degradable polymers, which form micelles in selective solvents, allowing for the creation of particles with a hydrophilic shell and hydrophobic core or vice versa, enabling targeted delivery and sequestration of agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional block copolymers are used, then structural simplicity is maintained, but ability to form amphiphilic micelles for selective solubilization is insufficient

Engineering Contradiction:
Improveability to form amphiphilic micellesVSAvoidcopolymer structure complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The copolymer is divided into distinct hydrophilic and hydrophobic blocks that self-assemble into micelles with separate core and shell regions, enabling selective solubilization of different substances

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention combines polysaccharide-based hydrophilic blocks with synthetic hydrophobic blocks to create amphiphilic copolymers that exhibit both water solubility and oil solubilization capabilities in micellar structures

Inventive Principle:
Principle #40Composite materials

2Reliability

If polysaccharide-based hydrophilic blocks are used, then biocompatibility and renewable resource utilization are improved, but synthesis complexity increases

Engineering Contradiction:
ImprovebiocompatibilityVSAvoidsynthesis process simplicity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

Activators and coupling agents are used as intermediaries to facilitate the chemical bonding between polysaccharide hydroxyl groups and polyester carboxyl groups, enabling efficient copolymer synthesis

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The synthesis process utilizes changes in pH, temperature, and solvent conditions to control the polymerization reaction and micelle formation, optimizing both biocompatibility and manufacturing efficiency

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If micelles with hydrophobic cores are formed, then solubilization of hydrophobic drugs is improved, but delivery across biological barriers becomes more challenging

Engineering Contradiction:
Improvedrug loading capacityVSAvoidbarrier penetration difficulty
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The micelle structure is designed with specific local properties: hydrophobic cores for drug loading and hydrophilic shells for biological compatibility and barrier penetration, optimizing both drug capacity and delivery efficiency

Inventive Principle:
Principle #3Local quality

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

These particles provide non-invasive, localized delivery of pharmaceutical and nutraceutical agents to the brain and efficient removal of substances like bile acids and toxins, with enhanced biocompatibility and renewable resource utilization.

Implementation Method 1

The amphiphilic block copolymers do not form a true solution in water and are able to form micelles in a selective solvent such as water

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

an amphiphilic linear block copolymer including a first polymer block and a second polymer block, wherein the first polymer block includes a polysaccharide or derivative

Methodology Applied
Scientific EffectAmphiphilic behavior: Amphiphiles

Data Source

PatentUS7763663B2Polysaccharide-containing block copolymer particles and uses thereof
Publication Date: 2010.07.27 MASSACHUSETTS UNIV OF
  • US7763663B2 patent drawing
  • US7763663B2 patent drawing
  • US7763663B2 patent drawing

AI summary

The invention relates to new amphiphilic linear block copolymers of polysaccharides and polymers. The amphiphilic linear block copolymers do not form a true solution in water and are able to form micelles in selective solvents. Also disclosed are particles, each of which has a shell and a core, and a diameter of about 1 to 1,000 nanometers, and methods of delivering agents or removing substances, e.g., undesirable substances, from a subject or environment, by using these particles.