Cationic Lipid Composition for Low-Cytotoxicity Drug Delivery

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Solution Overview

Problem

Existing cationic lipids and polycationic polymers used for drug delivery face issues such as cytotoxicity, complexity in synthesis, and low efficiency of intracellular nucleic acid delivery, while viral carriers pose risks like non-specific immune responses and high production costs.

Innovation Solution

A cationic lipid with a specific structure, represented by formula (1), that can easily form a complex with anionic drugs, allowing for efficient drug delivery through electrostatic interaction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cationic lipids are used for drug delivery, then they can form complexes with anionic drugs, but they exhibit cytotoxicity and have complicated synthesis methods

Engineering Contradiction:
Improvedrug delivery efficiencyVSAvoidcytotoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of cationic lipids by changing specific parameters (introducing specific functional groups at defined positions in the molecule) to alter their properties. This allows maintaining complex-forming capability while reducing cytotoxicity through structural optimization rather than complete redesign

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite lipid structure combining different functional groups (hydrophobic tail, hydrophilic head, and specific functional groups at defined positions) to achieve both effective drug complexation and reduced cytotoxicity through synergistic properties of the composite molecular structure

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional cationic lipids are used for drug delivery, then they can stabilize anionic drugs, but intracellular delivery efficiency is low

Engineering Contradiction:
Improvedrug stabilizationVSAvoidintracellular delivery efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies local quality modification by introducing specific functional groups at specific positions (R3, R4-R11) of the lipid molecule to enhance local interactions with cell membranes and intracellular structures, thereby improving intracellular delivery efficiency while maintaining overall drug stabilization capability

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention enhances the dynamic interaction between the cationic lipid and cell membranes through flexible molecular structures and specific functional groups that can adapt to membrane curvature and composition, facilitating more efficient intracellular delivery compared to rigid conventional structures

Inventive Principle:
Principle #15Dynamics

3Reliability

If polycationic polymers are used for drug delivery, then they can form complexes with nucleic acids, but they exhibit cytotoxicity due to multivalent cationic charges

Engineering Contradiction:
Improvenucleic acid deliveryVSAvoidcytotoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the charge density parameter by using monovalent or divalent cationic lipid molecules instead of multivalent polycationic polymers, while compensating through optimized lipid structure to maintain effective complex formation with nucleic acids at lower, more biocompatible charge densities

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 cationic lipid effectively forms complexes with anionic drugs, facilitating targeted delivery into living tissues with reduced cytotoxicity and improved efficiency.

Implementation Method 1

a cationic lipid or polycationic polymer stabilizes anionic drug by forming a complex through electrostatic interaction with the anionic drug

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Data Source

PatentEP4617258A1Cationic lipids and manufacturing method therefor
Publication Date: 2025.09.17 SAMYANG HLDG CORP
  • EP4617258A1 patent drawingFigure 1~2
  • EP4617258A1 patent drawingFigure 3~4
  • EP4617258A1 patent drawingFigure 5~6

AI summary

The present invention relates to cationic lipids and a manufacturing method therefor. More specifically, the present invention is concerned with cationic lipids that can easily form complexes with anionic drugs and thus are useful for drug delivery, and a method for manufacturing same.