Polyol-Modified Lipid Compounds for Stable Nucleic Acid Delivery

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Solution Overview

Problem

Existing nucleic acid delivery systems, such as lipid nanoparticles, face challenges in efficiently delivering nucleic acids to target cells due to rapid degradation and clearance, and variations in polyethylene glycol-based lipids affect drug stability and efficacy.

Innovation Solution

A polyglycol-modified lipid compound is developed, comprising specific structures and reactive groups, which is combined with cationic, neutral, and steroidal lipids to form lipid compositions for stable nucleic acid delivery, enhancing stability and efficiency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If polyethylene glycol-based lipids are used in lipid nanoparticles, then delivery efficiency is improved, but batch variations and quality stability deteriorate

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidbatch variations

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent changes the molecular weight parameter of PEG to a specific range (2000-5000 Da) and controls the PEG chain length (n=30-90), which standardizes the polymer structure and reduces batch variations while maintaining delivery efficiency

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite lipid structure by conjugating PEG with specific lipid moieties (such as distearoyl sn-glycero-3-phosphoethanolamine), combining the benefits of PEGylation with the stability of defined lipid structures to reduce batch variations

Inventive Principle:

Principle #40Composite materials

2Productivity

If polyethylene glycol-based lipids are used in lipid nanoparticles, then delivery efficiency is improved, but drug stability and efficacy deteriorate

Engineering Contradiction:

Improvedelivery efficiencyVSAvoiddrug stability

Core Design Contradiction:

ProductivityVSStability of the object's composition

Solution Approach 1:

The patent optimizes the PEG molecular weight to 2000-5000 Da and controls the number of repeating units (n=30-90), which provides optimal balance between steric protection (improving stability) and delivery efficiency

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The PEG-lipid conjugate acts as an intermediary that provides steric stabilization to the lipid nanoparticle surface, preventing aggregation and improving drug stability while maintaining delivery efficiency

Inventive Principle:

Principle #24Intermediary (Mediator)

3Ease of operation

If nucleic acids are delivered using conventional systems, then delivery capability is achieved, but rapid degradation and clearance occur

Engineering Contradiction:

Improvedelivery capabilityVSAvoidresistance to degradation

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses a lipid nanoparticle shell composed of PEG-lipid conjugates that provides flexible steric protection to the encapsulated nucleic acids, preventing nuclease degradation and reducing clearance while maintaining delivery capability

Inventive Principle:

Principle #30Flexible shells and thin films

Data Source

PatentEP4365168B1Polyol-modified lipid compound and preparation method and application thereof

Publication Date: 2025.10.15 JENKEM TECH CO LTD TIANJIN

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AI summary

Provided are a polyol-modified lipid compound, a preparation method therefor and an application thereof. The lipid compound and lipid nanoparticles prepared therefrom can target and effectively deliver biologically active substances to target cells and sites, and efficiently achieve pharmacological effects of the biologically active substances. In addition, the lipid compound has a singular molecular weight, which is beneficial for controlling differences between batches, improving the stability of finished drugs, and reducing immunogenicity; it is expected to be used for the development and application of related drugs.