Surface-Crosslinked Micelle Nanoparticles for Targeted Drug Delivery

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Solution Overview

Problem

Current cancer therapies face challenges due to the severe side effects of anticancer drugs, which often target healthy cells, and there is a need for improved methods to deliver therapeutic agents effectively, particularly for conditions involving multivalent interactions.

Innovation Solution

The development of stable nanoparticles using surface-crosslinked micelles that can encapsulate drugs and release them specifically at tumor sites, utilizing click chemistry to create multivalent ligands for targeted drug delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anticancer drugs are used to treat cancer, then therapeutic effectiveness is improved, but severe side effects occur due to targeting healthy cells

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidside effects on healthy cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention segments the drug delivery system into distinct components: a carrier vehicle (micelle or liposome) that transports the drug and a targeting ligand that directs the carrier to cancer cells. This segmentation allows the drug to be delivered specifically to the target, reducing exposure of healthy cells to the therapeutic agent and thereby reducing side effects while maintaining effectiveness.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention introduces a carrier vehicle (micelle or liposome) as an intermediary between the anticancer drug and the target cells. This intermediary carries the drug to the cancer cells through passive or active targeting mechanisms, enabling controlled release at the target site and minimizing direct contact with healthy cells, thus reducing side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If multivalent ligands are developed to enhance binding to cancer cells, then targeted delivery effectiveness is improved, but complexity of ligand structure increases

Engineering Contradiction:
Improvebinding effectivenessVSAvoidligand structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention merges multiple ligand units onto a single carrier surface to create a multivalent configuration. Instead of developing increasingly complex single-molecule ligands, the invention combines multiple simpler ligand units on the carrier surface, achieving enhanced binding effectiveness through multivalent interactions while keeping individual ligand structures relatively simple.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention transitions from considering ligand complexity in terms of molecular structure to considering it in terms of spatial arrangement. By organizing multiple ligand units on the two-dimensional surface of a carrier, the invention achieves multivalent binding effectiveness without proportionally increasing the complexity of individual ligand molecules, effectively adding a spatial dimension to the solution.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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 nanoparticles provide a controlled and targeted delivery of drugs, reducing side effects by releasing therapeutic agents specifically at cancerous tissues, enhancing the effectiveness of cancer therapy while minimizing harm to healthy cells.

Implementation Method 1

surfactants to form micelles

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

surface-crosslinked micelles prepared from surfactants

Methodology Applied
Scientific EffectAmphiphilic behavior: Amphiphiles

Implementation Method 3

crosslinking agents, wherein the crosslinking agents comprise two or more azido groups or two or more alkynyl groups; and inducing cycloaddition between the alkynes and azides

Methodology Applied
Scientific EffectClick chemistry: Chemical Bonding

Implementation Method 4

Hydrophobic guests can be encapsulated inside the SCMs

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Data Source

PatentUS10188605B2Nanoparticles and nanoparticle compositions
Publication Date: 2019.01.29 IOWA STATE UNIV RES FOUND INC
  • US10188605B2 patent drawing
  • US10188605B2 patent drawing
  • US10188605B2 patent drawing

AI summary

The invention provides multivalent surface-crosslinked micelle (SCM) particles, crosslinked reverse micelle (CRM) particles, and methods of making and using them. The SCM particles can be used, for example, to inhibit a virus or bacteria from binding to a host cell. The inhibition can be used in therapy for the flu, cancer, or AIDS. The CRM particles can be used, for example, to prepare metal nanoparticles or metal alloy nanoparticles, or they can be used in catalytic reactions.