Amphiphilic Polymers Forming Multi-Micellar Structures for Targeted Drug Delivery

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Solution Overview

Problem

Current drug delivery systems face challenges in achieving targeted and controlled release of therapeutically active agents, particularly in cancer treatment, where they often result in harmful effects on normal cells and lack stability and biocompatibility.

Innovation Solution

Development of amphiphilic polymeric compositions that form multi-micellar structures with a hydrophobic and hydrophilic domain, capable of binding to carbohydrate cell receptors, allowing for targeted accumulation in cancer cells and reducing toxicity through encapsulation and controlled release of active agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If conventional drug delivery systems are used, then drug release can be achieved, but harmful effects on normal cells occur and stability is poor

Engineering Contradiction:
Improveharmful effects on normal cellsVSAvoidstability
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The system segments the drug delivery function into distinct components: amphiphilic polymers self-assemble into micelles with hydrophobic cores for drug loading and hydrophilic shells for stability. This segmentation allows the drug to be isolated within the micelle structure, reducing harmful effects on normal cells while maintaining systemic stability during circulation.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The micelle structure provides local quality differentiation with a hydrophobic interior for encapsulating therapeutic agents and a hydrophilic exterior for aqueous compatibility and stability. The hydrophilic shell specifically interacts with the aqueous environment to maintain stability, while the hydrophobic core locally concentrates the therapeutic agent for targeted release.

Inventive Principle:
Principle #3Local quality

2Reliability

If targeted accumulation in cancer cells is achieved through receptor binding, then efficacy increases, but device complexity increases

Engineering Contradiction:
ImproveefficacyVSAvoidstructure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The amphiphilic polymers exhibit self-service behavior by automatically self-assembling into micellar structures when exposed to aqueous environments. This self-assembly process occurs spontaneously without requiring external guidance or complex assembly mechanisms, thereby achieving targeted accumulation functionality while minimizing structural complexity.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The system utilizes parameter changes in the polymer structure (amphiphilic balance, molecular weight, composition ratios) to control micelle formation, size, and stability. By adjusting these parameters, the system achieves optimal targeted accumulation and efficacy without requiring complex structural designs, as the self-assembly process naturally optimizes the micelle properties based on the polymer parameters.

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 amphiphilic polymeric compositions effectively increase the accumulation of therapeutically active agents in target cells while minimizing off-target effects, enhancing efficacy and reducing toxicity, thereby improving the treatment of medical conditions such as cancer.

Implementation Method 1

the one or more amphiphilic copolymers are configured to form a multi-micellar structure

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

amphiphilic copolymers comprises a hydrophobic domain and a hydrophilic domain

Methodology Applied
Scientific EffectAmphiphilic aggregation: Amphiphiles

Implementation Method 3

at least a portion of the hydrophilic domain is capable of binding to a cell or a cell organelle via a carbohydrate cell receptor and/or transporter

Methodology Applied
Scientific EffectSpecific binding: Adsorption

Data Source

PatentUS20210115177A1Amphiphilic polymers, process of preparing same and uses thereof
Publication Date: 2021.04.22 TECHNION RES & DEV FOUND LTD
  • US20210115177A1 patent drawing
  • US20210115177A1 patent drawing
  • US20210115177A1 patent drawing

AI summary

Compositions comprised of an amphiphilic block polymer, configured to form multi-micellar structures having hydrophilic and hydrophobic domains, and uses same for encapsulating therein active agents such as hydrophobic therapeutic agents, are disclosed. The disclosed compositions are useful e.g., for orally delivering the active agent encapsulated therein and may further be used for controllably releasing the agents in the physiological environment.