Polymer-Copper Nanoparticles for Selective Cancer Cell Targeting

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Solution Overview

Problem

Current anticancer drugs face challenges due to drug resistance and poor selectivity, leading to side effects on healthy tissues, as they often target rapidly proliferating cells, including normal cells, and have limited effectiveness in eradicating cancer cells without damaging healthy tissue.

Innovation Solution

A polymer/copper combination, specifically a biocompatible copolymer with pyridine-2-thiol side groups and copper ions, forms nanoparticles with a hydrophilic exterior, allowing targeted delivery and uptake by cancer cells, where copper ions induce cell death through interaction with intracellular thiols and glutathione, while sparing normal cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional anticancer drugs are used to target rapidly proliferating cancer cells, then cancer cell proliferation is inhibited, but normal fast-growing cells are also damaged causing side effects

Engineering Contradiction:
Improveanticancer efficacyVSAvoidside effects on healthy tissue
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The copolymer is designed with dual functionality: pyridine-2-thiol side groups that selectively bind copper ions and interact with cancer cell thiols, and hydrophilic blocks that provide water solubility and biocompatibility. This local differentiation of polymer properties enables selective cancer cell targeting while minimizing damage to normal cells.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention combines organic copolymer material with copper ions to create a composite therapeutic agent. The copolymer-copper complex leverages both the polymer's targeting capabilities and copper's cytotoxic effects, achieving enhanced cancer cell killing with reduced off-target effects compared to traditional single-agent therapies.

Inventive Principle:
Principle #40Composite materials

2Reliability

If copper chelators are used to deplete copper levels in tumors, then angiogenesis is inhibited and cancer cells are killed, but the chelators are rapidly cleared and show little overall benefit

Engineering Contradiction:
Improveanti-angiogenesis efficacyVSAvoidcirculation time of chelator
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The copolymer acts as an intermediary carrier that delivers copper ions to tumor tissues. Rather than using small molecule chelators that are rapidly cleared, the polymer-copper complex provides sustained copper delivery, with the polymer protecting the copper ions and enabling prolonged circulation and tumor accumulation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical and chemical parameters of copper delivery by complexing copper ions with the copolymer. This transformation increases the molecular size and hydrophilicity, reducing renal clearance and extending circulation time, while the pyridine-2-thiol groups maintain copper binding affinity for targeted delivery to cancer cells.

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If anticancer drugs are designed to be highly selective for cancer cells, then side effects are reduced, but drug resistance develops limiting long-term effectiveness

Engineering Contradiction:
Improveside effects on healthy tissueVSAvoidlong-term anticancer effectiveness
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The copolymer combines multiple anti-cancer mechanisms in one agent: copper ion binding and delivery, direct thiol interaction with cancer cells, and induction of oxidative stress. This multi-modal approach addresses cancer cells through several pathways simultaneously, making it harder for cells to develop resistance compared to single-mechanism therapies.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The copolymer structure incorporates universal cancer-targeting features: pyridine-2-thiol groups that bind copper and interact with thiols (present in all cancer cells), hydrophilic blocks for circulation, and the ability to generate reactive oxygen species. This multi-functional design broadens the therapeutic window and reduces selectivity-dependent resistance.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 polymer/copper combination selectively kills cancer cells, including drug-resistant cells, with minimal side effects on normal cells, due to differences in intracellular glutathione levels and gene expression, offering a broad-spectrum anticancer activity with enhanced efficacy and prolonged circulation time.

Implementation Method 1

copper ions induce cell death through interaction with intracellular thiols and glutathione

Methodology Applied
Scientific EffectChemical interaction with thiols: Chemical Bonding

Implementation Method 2

The polymer/copper combination can be in the form of a particle, e.g., a nanoparticle, with the hydrophilic component at the exterior surface of the particle

Methodology Applied
Scientific EffectHydrophilic interaction: Hydrophile

Data Source

PatentUS10221271B2Polymer/copper combination for targeted cancer therapy
Publication Date: 2019.03.05 UNIVERSITY OF SOUTH CAROLINA
  • US10221271B2 patent drawing
  • US10221271B2 patent drawing
  • US10221271B2 patent drawing

AI summary

Polymer/copper combinations that can selectively target and kill cancer cells are described. Materials can include the reaction product of a biocompatible hydrophilic polymer and pyridine-2-thiol containing monomer. The copolymer reaction product can include pyridine-2-thiol side groups pendant to the backbone via a disulfide linkage. The hydrophilic component can form the polymer backbone and/or can form hydrophilic pendant groups off of the backbone. Copper ions can be associated with the copolymer.