Ceramic Nanoparticles for siRNA Delivery

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Solution Overview

Problem

Current siRNA therapy faces challenges such as enzymatic degradation, poor cellular penetration, and low efficacy due to difficulties in delivering biomolecules like siRNA across cellular membranes without causing immunological reactions or exposing them to degradation, which limits its therapeutic effectiveness and increases costs.

Innovation Solution

Development of particulate substances comprising a ceramic matrix with an aminofunctional group that promotes cell penetration and encapsulates biomolecules within pores, protecting them from degradation until release in the cytoplasm, using a process involving emulsion formation and ceramic precursor hydrolysis to create particles with controlled release properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If siRNA is delivered using viral vectors, then delivery efficiency is improved, but immunological reactions and difficulty in implementation occur

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidimmunological reactions
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses non-viral ceramic nanoparticles as disposable delivery vehicles that avoid immunological reactions. These particles are designed for single-use delivery without the persistence and immune recognition issues of viral vectors, achieving effective siRNA delivery without triggering harmful immune responses

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Ease of operation

If siRNA is adsorbed onto nanoparticle surfaces, then delivery is enabled, but enzymatic degradation occurs prior to delivery

Engineering Contradiction:
Improvedelivery capabilityVSAvoidprotection from enzymatic degradation
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent embeds siRNA molecules within the porous interior structure of ceramic nanoparticles, nesting the biomolecule inside the particle matrix rather than adsorbing it on the surface. This internal positioning protects the siRNA from enzymatic degradation in the extracellular environment while maintaining delivery capability

Inventive Principle:
Principle #7Nested doll (Nesting)

Solution Approach 2:

The patent utilizes porous ceramic nanoparticles with controlled pore structures that can accommodate and protect siRNA molecules. The porous matrix provides both protection from degradation and pathways for cellular uptake and intracellular release

Inventive Principle:
Principle #31Porous materials

3Reliability

If siRNA is encapsulated within porous ceramic particles, then protection from degradation is achieved, but homogeneous distribution of aminofunctional groups is required for effective penetration

Engineering Contradiction:
Improveprotection from degradationVSAvoidhomogeneous distribution of functional groups
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent employs controlled hydrolysis and condensation parameters during ceramic particle synthesis to ensure uniform distribution of aminofunctional groups throughout the particle matrix. By optimizing pH, temperature, and precursor ratios, homogeneous functional group distribution is achieved, enabling effective cellular penetration while maintaining protection

Inventive Principle:
Principle #35Parameter changes

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 ceramic matrix particles effectively protect and deliver biomolecules, enhancing therapeutic efficacy by preventing enzymatic degradation and facilitating cellular uptake and release, potentially reducing treatment costs and improving clinical outcomes.

Implementation Method 1

particles of a ceramic matrix bearing an aminofunctional group, the aminofunctional group being capable of promoting penetration of the particles into cells

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Implementation Method 2

a biomolecule disposed within pores of the particles, the biomolecule being releasable from the particles by dissolution of the ceramic matrix

Methodology Applied
Scientific EffectPhysical containment: Physical Containment

Implementation Method 3

the biomolecule being releasable from the particles by dissolution of the ceramic matrix

Methodology Applied
Scientific EffectDissolution:

Data Source

PatentEP2605755B1Particulate substances comprising ceramic particles for delivery of biomolecules
Publication Date: 2019.07.31 AUSTRALIAN NUCLEAR SCI & TECH ORGANISATION
  • EP2605755B1 patent drawingFigure 1
  • EP2605755B1 patent drawingFigure 2~3
  • EP2605755B1 patent drawingFigure 4

AI summary

A particulate substance comprising particles of a ceramic matrix bearing a functional group, the functional group being capable of promoting penetration of the particles into cells, and a biomolecule disposed within pores of the particles, the biomolecule being releasable from the particles by dissolution of the ceramic matrix.