Lipid Nanoparticle Formulation for mRNA Encapsulation and Tissue Targeting

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing lipid nanoparticle formulations for mRNA delivery require optimization of multiple lipids, which can affect diameter, encapsulation, zeta potential, and tissue targeting, necessitating the development of alternative lipid structures for improved nucleic acid delivery.

Innovation Solution

A novel compound of Formula I, which can be used in lipid nanoparticles, combined with other lipid components, to enhance the delivery of therapeutic agents such as mRNA, offering flexibility in tissue targeting and encapsulation efficiency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If classical lipid formulations are used with multiple lipids, then encapsulation of nucleic acids is achieved, but the formulation requires individual optimization of each lipid and cannot easily target specific tissues

Engineering Contradiction:

Improveencapsulation of nucleic acidsVSAvoidtissue targeting flexibility

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of the ionizable lipid by changing parameters such as the ring structure (cycloalkyl, heterocyclyl, aryl, or heteroaryl), chain length (C1-20 alkyl), and functional groups to create a library of lipids with different tissue targeting properties while maintaining nucleic acid encapsulation capability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent combines the novel ionizable lipid with helper lipids, cholesterol, and PEG-lipids to create composite lipid nanoparticle formulations that leverage the encapsulation efficiency of classical formulations while adding tissue targeting capabilities through the modified lipid structure

Inventive Principle:

Principle #40Composite materials

2Reliability

If multiple lipids are used in classical formulations, then nucleic acid delivery is achieved, but the diameter, encapsulation, zeta potential, and tissue targeting require individual optimization

Engineering Contradiction:

Improvenucleic acid deliveryVSAvoidformulation optimization complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The novel ionizable lipid is designed to perform multiple functions simultaneously: it provides nucleic acid encapsulation, maintains appropriate zeta potential, controls nanoparticle diameter, and enables tissue targeting, thereby reducing the need for individual optimization of separate lipid components

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Adaptability or versatility

If alternative lipid structures are developed, then tissue targeting flexibility is improved, but the encapsulation efficiency and delivery performance require further optimization

Engineering Contradiction:

Improvetissue targeting flexibilityVSAvoidencapsulation efficiency

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent introduces specific functional groups and structural features at localized positions within the lipid molecule (such as substituents on the ring structure or at specific positions in the alkyl chain) to enhance tissue targeting while preserving the hydrophobic and hydrophilic regions necessary for nucleic acid encapsulation

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS12599560B2Lipids and lipid nanoparticle formulations

Publication Date: 2026.04.14 SHENZHEN LONGUIDE BIOPHARMA CORP

AI summary

The present disclosure relates generally to lipids, lipid nanoparticle formulations, and methods of using the same for delivering nucleic acids, such as mRNA.