Nanoscale Coordination Polymer Carriers for Co-Delivery

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Solution Overview

Problem

Current delivery systems for nucleic acids and photosensitizers face challenges such as vulnerability to degradation, transient effects, and low delivery efficiency, particularly in cancer therapy, where targeted and combined delivery of these therapeutics is needed to overcome drug resistance and enhance treatment efficacy.

Innovation Solution

A nanoscale particle platform utilizing a metal-organic matrix material with a core comprising a metal bisphosphonate coordination polymer and a lipid bilayer coating for co-delivery of chemotherapeutics and nucleic acids, including siRNAs, to enhance anticancer therapy by improving stability, targeting, and synergistic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If nucleic acids are administered directly, then therapeutic effects can be achieved, but they are vulnerable to degradation by enzymes and have transient effects

Engineering Contradiction:
Improvestability of nucleic acidsVSAvoidduration of therapeutic effect
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent applies preliminary action by pre-encapsulating nucleic acids in nanoscale coordination polymer particles before administration. This preliminary encapsulation protects the nucleic acids from enzymatic degradation in the bloodstream and enables prolonged circulation, thereby extending the duration of therapeutic effect while maintaining stability.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The nanoscale coordination polymer particles serve as an intermediary carrier between the nucleic acids and the biological environment. This intermediary structure protects the vulnerable nucleic acids from direct exposure to degrading enzymes while facilitating their delivery to target cells, thus improving both reliability and duration of action.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If existing delivery systems are used for nucleic acids, then some delivery can be achieved, but delivery efficiency is low and circulation is not prolonged

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidcirculation time
Core Design Contradiction:
ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent employs composite materials by creating nanoscale particles with a coordination polymer core and a lipid bilayer shell. This composite structure combines the advantages of both materials: the coordination polymer provides structural stability and controlled release, while the lipid bilayer enhances biocompatibility and circulation time, thereby improving both delivery efficiency and duration of action.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent applies parameter changes by optimizing the size, surface charge, and composition of the nanoscale particles to enhance their circulation properties. By controlling particle size in the nanoscale range and adjusting surface characteristics, the system achieves prolonged circulation in the bloodstream while maintaining high delivery efficiency to target cells.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If single therapeutic agents are delivered, then specific therapeutic effects are achieved, but drug resistance occurs and treatment efficacy is limited

Engineering Contradiction:
Improvetreatment efficacyVSAvoidability to overcome drug resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies merging by combining multiple therapeutic agents (nucleic acids and chemotherapeutic drugs) into a single nanoscale delivery system. This co-delivery approach enables synergistic therapeutic effects while overcoming drug resistance, as the combined agents attack cancer cells through multiple mechanisms simultaneously, improving overall treatment efficacy and adaptability.

Inventive Principle:
Principle #5Merging (Combining)

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 platform achieves enhanced stability and targeted delivery of multiple therapeutics, promoting prolonged circulation, improved cellular uptake, and synergistic anticancer effects, effectively addressing limitations in existing delivery methods.

Implementation Method 1

the metal-organic matrix material core comprises a metal bisphosphonate coordination polymer comprising a multivalent metal ion and a bisphosphonate

Methodology Applied
Scientific EffectCoordination polymer formation: Chemical Bonding

Implementation Method 2

A nanoscale particle platform utilizing a metal-organic matrix material with a core comprising a metal bisphosphonate coordination polymer and a lipid bilayer coating

Methodology Applied
Scientific EffectLipid bilayer formation: Amphiphiles

Data Source

PatentEP3065713B1Nanoscale carriers for the delivery or co-delivery of chemotherapeutics, nucleic acids and photosensitizers
Publication Date: 2024.03.06 UNIVERSITY OF CHICAGO
  • EP3065713B1 patent drawingFigure 1
  • EP3065713B1 patent drawingFigure 2
  • EP3065713B1 patent drawingFigure 3a)~3c)

AI summary

Nanoscale coordination polymer nanoparticles for the co-delivery of multiple therapeutic agents are described. The multiple therapeutic agents can include a combination of different chemotherapeutic agents, a combination of one or more chemotherapeutic agents and one or more nucleic acids, such as small interfering RNA (siRNA) or microRNA, a combination of one or more chemotherapeutic agents and a photosensitizer (i.e., for use in photodynamic therapy), or a plurality of different siRNAs. Pharmaceutical formulations including the nanoparticles, methods of using the nanoparticles to treat cancer, and methods of making the nanoparticles are also described.