Cationic Cholesterol Lipid Nanoparticles for Local mRNA Retention

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Solution Overview

Problem

Existing lipid nanoparticles for nucleic acid delivery, such as those used in COVID-19 vaccines, cause systemic reactions and myocarditis due to widespread distribution in the body, necessitating a delivery carrier that confines mRNA expression to the injection site and minimizes systemic distribution.

Innovation Solution

Lipid nanoparticles comprising cationic cholesterol, ionizable lipid, cholesterol, helper lipid, and PEG lipid, with specific molar ratios, to confine nucleic acid delivery to the site of administration and increase protein expression duration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional lipid nanoparticles are used for nucleic acid delivery, then the nucleic acid can be delivered to the body, but the nanoparticles spread throughout the body causing systemic reactions and myocarditis

Engineering Contradiction:

Improvenucleic acid deliveryVSAvoidsystemic reactions and myocarditis

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the lipid nanoparticle composition to create local quality differences in distribution and retention. By incorporating specific lipids and adjusting composition ratios, the nanoparticles achieve preferential accumulation and prolonged retention at the injection site while reducing systemic spread, thereby delivering nucleic acid locally without causing widespread systemic reactions

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent changes physical and chemical parameters of the lipid nanoparticle system, including lipid composition ratios, particle size, and surface properties. These parameter modifications alter the biodistribution profile, enabling the nanoparticles to remain confined to the injection site longer and reduce systemic circulation, thus preventing myocarditis while maintaining delivery efficacy

Inventive Principle:

Principle #35Parameter changes

2Duration of action of moving object

If mRNA is delivered systemically, then broad distribution occurs, but the duration of protein expression decreases due to rapid clearance

Engineering Contradiction:

Improveprotein expression durationVSAvoidtherapeutic dose utilization

Core Design Contradiction:

Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The patent employs preliminary action by pre-modifying the lipid nanoparticle composition before administration to enhance local retention. The optimized lipid formulation prepares the nanoparticles to accumulate and persist at the injection site, creating a reservoir that slowly releases nucleic acid over time, thereby extending protein expression duration without requiring increased dosing

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS20250381140A1Lipid nanoparticles using cationic cholesterol for local delivery for nucleic acid delivery

Publication Date: 2025.12.18 GC BIOPHARMA CORP

AI summary

The present invention is directed to lipid nanoparticles using cationic cholesterol for topical delivery for nucleic acid delivery, and when administered locally, side effects caused by systemic drug delivery can be minimized and protein expression can be confined to the site of administration. In addition, the duration of protein expression at the site of administration can be increased, and thus the lipid nanoparticles can be useful in the technical field related to nucleic acid therapeutics.