Amphiphilic Dendron-Coil Micelles for Targeted Drug Delivery

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Solution Overview

Problem

Current drug delivery systems face challenges in targeting specific cells, such as cancer cells, and efficiently capturing circulating tumor cells, which are rare in the bloodstream, making effective drug delivery and detection difficult.

Innovation Solution

Amphiphilic dendron-coils, comprising a non-peptidyl hydrophobic core-forming block, a polyester dendron, and a poly(ethylene) glycol moiety, self-assemble into micelles that can encapsulate drugs and conjugate with targeting ligands for enhanced cell specificity and circulation time, facilitating both drug delivery and cell capture.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional drug delivery systems are used, then drugs can be administered to patients, but they cannot effectively target specific cells or capture circulating tumor cells

Engineering Contradiction:
Improvetargeting efficacyVSAvoiddetection efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The system segments the drug delivery function into distinct modular components: amphiphilic dendron-coils that self-assemble into micelles, ligand molecules for target recognition, and therapeutic agents. This modular architecture enables independent optimization of targeting and drug delivery functions, improving both reliability and productivity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention uses composite micelle structures formed by amphiphilic dendron-coils containing both hydrophobic core-forming blocks and hydrophilic PEG blocks. This composite material design enables simultaneous drug encapsulation, circulation stability, and target-specific binding, resolving the contradiction between general drug delivery and specific cell targeting.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If micelles are used for drug delivery, then drugs can be protected and delivered, but circulation time is limited

Engineering Contradiction:
Improvecirculation timeVSAvoidtargeting specificity
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The dendron-coil architecture implements local quality differentiation with hydrophobic core blocks for drug encapsulation and protection, and hydrophilic PEG blocks for circulation stability. This spatial separation of functions extends circulation time while maintaining targeting capability through ligand conjugation.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The PEG blocks act as intermediaries between the hydrophobic drug core and the aqueous bloodstream environment, providing steric stabilization and extending circulation time. Simultaneously, ligand intermediaries on the micelle surface mediate specific binding to target cells, resolving the contradiction between circulation duration and targeting specificity.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of operation

If circulating tumor cells are detected using conventional methods, then some detection can be achieved, but the process is invasive and time-consuming

Engineering Contradiction:
Improvesampling simplicityVSAvoiddetection efficiency
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The micelle system performs self-directed targeting and capture of circulating tumor cells through ligand-receptor binding, eliminating the need for complex invasive procedures. Simple blood sampling followed by micelle incubation enables efficient CTC capture, improving both ease of operation and detection efficiency.

Inventive Principle:
Principle #25Self-service

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 dendron-coil micelles provide controlled drug release, prolonged circulation, and enhanced targeting efficacy, enabling efficient delivery of drugs to specific cells and capturing of circulating tumor cells, improving cancer treatment and diagnosis.

Implementation Method 1

Self-assembly is a process in which a stable ordered ensemble of molecules is formed through the balancing of attractive and repulsive forces between amphiphiles at a concentration above the critical micelle concentration (CMC).

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

Each amphiphilic dendron-coil comprises a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Data Source

PatentEP2678042B1Amphiphilic dendron-coils, micelles thereof and uses
Publication Date: 2018.05.09 THE BOARD OF TRUSTEES OF THE UNIV OF ILLINOIS
  • EP2678042B1 patent drawingFigure 1
  • EP2678042B1 patent drawingFigure 2
  • EP2678042B1 patent drawingFigure 3

AI summary

The invention generally relates to the fields of drug delivery and cell capture. In particular, the invention relates to amphiphilic dendron-coils, micelles thereof and their use for drug delivery vehicles and/or cell capture.