Supramolecular Nanoparticles for Controlled Size and Stability

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Solution Overview

Problem

Current nanoparticle-based therapies face challenges in achieving controlled size, improved morphology, reduced toxicity, lower immune system side-effects, and enhanced stability, which limits their clinical application, particularly for viral infections and gene delivery.

Innovation Solution

Development of supramolecular nanoparticles composed of combinatorial carboxylated cobalamins, dipyridamoles, and basic amino acid polypeptides, which form dynamic self-organizing structures with binding and terminating components, allowing for controlled assembly and function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If traditional nanoparticle-based therapies are used, then delivery capability is achieved, but controlled size and stability are limited

Engineering Contradiction:
Improvenanoparticle size controlVSAvoidnanoparticle stability
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent employs dynamic combinatorial chemistry to create supramolecular nanoparticles that can self-adjust and self-heal. The system uses reversible non-covalent interactions (hydrogen bonding, metal coordination, hydrophobic forces) that allow the nanoparticle structure to dynamically adapt to environmental conditions while maintaining stable overall architecture, thus achieving both size control and stability.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The invention utilizes changes in physical and chemical parameters (pH, temperature, ionic strength) to control nanoparticle assembly and disassembly. By tuning these parameters, the system can precisely control nanoparticle size and stability in different physiological environments, resolving the contradiction between size control and stability.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If nanoparticle concentration is increased to improve therapeutic effect, then antiviral activity increases, but toxicity and immune system side-effects worsen

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtoxicity and immune side-effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The supramolecular nanoparticles are designed with specific surface properties and functional groups that enable selective interaction with viral particles while being biocompatible. The local chemical environment of the nanoparticle surface is optimized to achieve high antiviral activity at low concentrations, reducing systemic toxicity and immune responses.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses supramolecular assemblies as intermediaries that can reversibly bind viral particles. These intermediaries neutralize viruses through non-covalent interactions, providing therapeutic effect without the harsh conditions or high concentrations that would cause toxicity. The reversible nature allows for controlled release and reduced accumulation.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Loss of information

If simple molecular structures are used, then predictability is maintained, but supramolecular complexity and functionality are reduced

Engineering Contradiction:
Improvepredictability of molecular structureVSAvoidsupramolecular functionality
Core Design Contradiction:
Loss of informationVSAdaptability or versatility

Solution Approach 1:

The patent divides the supramolecular system into discrete functional modules (binding units, structural units, functional units) that can be independently designed and assembled. Each module has predictable behavior based on its molecular structure, while the overall supramolecular assembly achieves complex functionality through the organized combination of these modules.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates universal building blocks with multiple binding sites and functional groups that can participate in various non-covalent interactions. These multi-functional units can assemble into different supramolecular structures depending on conditions, providing both predictability through standardized components and versatility through configurable assemblies.

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 supramolecular nanoparticles demonstrate antiviral properties and improved delivery capabilities, offering a more efficient and targeted therapeutic approach with reduced toxicity and enhanced stability.

Implementation Method 1

combinatorial carboxylated cobalamins, and 2) combinatorial carboxylated dipyridamoles... which form dynamic self-organizing structures with binding and terminating components

Methodology Applied
Scientific EffectMolecular recognition:

Implementation Method 2

The study of non-covalent interactions is crucial to understanding many biological processes that rely on these forces for structure and function. Biological systems are often the inspiration for supramolecular research.

Methodology Applied
Scientific EffectNon-covalent interactions:

Implementation Method 3

chemists have mistakenly become complacent with paradigms of molecular structure... looking to chemical synthesis and composition utilities at the supramolecular level... molecular self-assembly

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Data Source

PatentEP3922347B1Supramolecular systems based on dynamic self-organizing nanostructures with antiviral properties
Publication Date: 2024.12.18 FARBER BORIS SLAVINOVICH
  • EP3922347B1 patent drawingFigure 1
  • EP3922347B1 patent drawingFigure 2
  • EP3922347B1 patent drawingFigure 3

AI summary

Methods of producing supramolecular structures using molecular recognition and methods of controlling the size of the nanoparticles produced to form discrete particles. Pharmaceutical formulations of the supramolecular structures for viral infections treatments. Supramolecular nanoparticles may comprise combinatorial carboxylated cobalamins; combinatorial carboxylated dipyridamoles; and basic amino acid polypeptides. The supramolecular nanoparticles are dynamic self-organizing soluble nanostructures which have a plurality of binding components, organic cores, and terminating components. The binding components include combinatorial carboxylated cobalamins with binding regions. The organic cores include combinatorial carboxylated dipyridamole adapted to bind to the combinatorial carboxylated cobalamins such that the organic cores can provide a mechanical structure for the self-organizing soluble nanostructures and a first type of inclusion complexes. The supramolecular nanoparticles include terminating components with at least one terminating binding element capable of binding to a residual binding region of a binding components.