Silicon Nanoparticle Composition for Controlled siRNA and mRNA Delivery

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Solution Overview

Problem

The delivery of siRNA and mRNA therapeutics is hindered by the inability to cross cell membranes, short in vitro half-life, high molecular weight, poor specificity and uptake in target tissues, cellular toxicity, and undesirable off-target effects, particularly in ocular tissues where ocular surface barriers and frequent treatment regimens increase the risk of complications.

Innovation Solution

A composition comprising silicon nanoparticles, at least one amino acid, and at least one lipid, with silicon nanoparticles comprising at least 50% by weight silicon, is used to deliver nucleic acids such as siRNA or mRNA, where the lipid surface treatment controls the zeta potential and rate of release, enhancing stability and cellular uptake.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If naked siRNA is used for delivery, then the therapeutic potential is maintained, but the ability to cross cell membranes is lost due to electrostatic repulsion from negative charges

Engineering Contradiction:

Improvetherapeutic potentialVSAvoidcell membrane crossing ability

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

Cationic lipids and amino acids are used as intermediary carriers to complex with negatively charged siRNA, forming positively charged nanocomplexes that can overcome electrostatic repulsion and facilitate cell membrane crossing while maintaining siRNA therapeutic activity

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The surface charge of the delivery system is changed from negative (naked siRNA) to positive (lipid-amino acid complex) by adjusting the composition ratios of cationic lipids and amino acids, enabling the system to cross cell membranes effectively

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If naked siRNA is administered, then the full therapeutic dose is available, but the in vitro half-life is shortened due to cellular and systemic defence mechanisms

Engineering Contradiction:

Improvetherapeutic dose availabilityVSAvoidin vitro half-life

Core Design Contradiction:

Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

A lipid-based protective shell is formed around siRNA through complexation with cationic lipids and amino acids, creating a stable nanocomplex that protects the siRNA from cellular and systemic defence mechanisms while allowing controlled release at the target site

Inventive Principle:

Principle #30Flexible shells and thin films

Solution Approach 2:

A composite delivery system is created by combining siRNA with cationic lipids and amino acids in specific ratios, forming a stable nanocomplex that provides both protection against degradation and facilitated cellular uptake

Inventive Principle:

Principle #40Composite materials

3Reliability

If high molecular weight siRNA is used, then the gene targeting capability is maintained, but the uptake in target tissues is reduced

Engineering Contradiction:

Improvegene targeting capabilityVSAvoidtarget tissue uptake

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The siRNA is complexed with lipid and amino acid components that segment the large molecular weight siRNA into smaller nanoscale complexes, improving penetration into target tissues while maintaining the intact siRNA sequence for gene targeting

Inventive Principle:

Principle #1Segmentation

4Reliability

If frequent topical treatment is applied to ocular surface, then the therapeutic effect is maintained, but the risk of complications increases due to ocular surface barriers

Engineering Contradiction:

Improvetherapeutic effectVSAvoidcomplication risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The lipid-amino acid-siRNA nanocomplex exhibits pH-responsive behavior that enables self-disassembly at the slightly acidic endosomal environment, automatically releasing siRNA into the cytoplasm without requiring frequent external application or intervention

Inventive Principle:

Principle #25Self-service

Solution Approach 2:

The flexible lipid-based shell provides protection during ocular surface transit and enables controlled release at the target site, reducing the frequency of application needed and thereby lowering complication risks

Inventive Principle:

Principle #30Flexible shells and thin films

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 composition allows for controlled release and improved delivery of siRNA and mRNA to target sites, including ocular tissues, with enhanced stability and reduced off-target effects, facilitating efficient gene silencing and treatment.

Implementation Method 1

the lipid surface treatment controls the zeta potential and rate of release, enhancing stability and cellular uptake

Methodology Applied

Scientific EffectZeta potential: Electrostatics

Implementation Method 2

the silicon nanoparticles comprise at least 50% by weight silicon

Methodology Applied

Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS12496278B2Delivery system comprising silicon nanoparticles

Publication Date: 2025.12.16 SISAF LTD

AI summary

A composition for the controlled release of a nucleic acid such as short interfering RNA or messenger RNA, comprising silicon nanoparticles, at least one amino acid, and at least one lipid, wherein the silicon nanoparticles comprise at least 50% by weight silicon. Also related compositions and methods.