Hydroxylated Polyamine RNA Transfection for Stable Cell Uptake

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Solution Overview

Problem

Existing transfection reagents face challenges in achieving a high signal-to-noise ratio and efficient transfection across a broad range of cell types, with many strategies failing to provide a clear rationale for improvement.

Innovation Solution

The use of polyamine derivatives chemically modified with hydroxylated substituents bonded via hydrophobic linkers and hydrophobic substituents, such as hydroxyalkyl-alkyl-polyamines, which enhance cellular uptake and stability of transfection complexes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If hydrophobic modifications are introduced to improve membrane penetration, then transfection efficiency is improved, but complex stability in solution deteriorates and aggregation occurs

Engineering Contradiction:
Improvetransfection efficiencyVSAvoidcomplex stability in solution
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by systematically varying the hydrophobicity parameters of polyamine derivatives. Specifically, it introduces hydroxylated substituents with different chain lengths (C4-C40) and hydrophobic substituents with controlled carbon numbers (2-40 carbons) and heteroatom compositions. This systematic parameter optimization allows the transfectant to achieve enhanced membrane penetration while maintaining solution stability by fine-tuning the balance between hydrophobic and hydrophilic characteristics.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating polyamine derivatives that combine multiple functional substituents on a single molecular framework. The composite structure includes: (1) a polyamine backbone providing cationic charge, (2) hydroxylated substituents with hydrophobic linkers for membrane interaction, and (3) additional hydrophobic substituents for enhanced penetration. This multi-functional composite design enables simultaneous achievement of complex stability and transfection efficiency.

Inventive Principle:
Principle #40Composite materials

2Measurement precision

If the signal-to-noise ratio is increased for better transfection specificity, then transfection quality is improved, but transfection efficiency across diverse cell types may deteriorate

Engineering Contradiction:
Improvesignal-to-noise ratioVSAvoidtransfection efficiency across cell types
Core Design Contradiction:
Measurement precisionVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by designing a polyamine derivative structure that performs multiple functions simultaneously: (1) forms stable complexes with RNA through cationic charge, (2) enhances membrane penetration through hydrophobic substituents, (3) maintains solution stability through hydroxylated groups, and (4) achieves broad cell type compatibility through optimized amphiphilic balance. This multi-functional design enables the single transfectant to work effectively across diverse cell types while maintaining high signal-to-noise ratio.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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

These modified polyamines achieve superior transfection efficiency with a high signal-to-noise ratio across various cell types, outperforming commercially available materials.

Implementation Method 1

Polyamines form polycations in solution, which facilitates the complex formation with polyanions such as nucleic acids.

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Implementation Method 2

each of said hydroxylated substituents comprises any one or more of the following moieties as said hydrophobic linker: alkylene, alkenylene, alkynylene, cycloalkylene, cycloalkenylene, arylene, and combinations thereof

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Data Source

PatentEP4085930B1Hydroxylated polyamine derivatives as transfection reagents for RNA
Publication Date: 2026.04.22 BIONTECH DELIVERY TECHNOLOGIES GMBH
  • EP4085930B1 patent drawingFigure 1~2
  • EP4085930B1 patent drawingFigure 3~4
  • EP4085930B1 patent drawing

AI summary

The invention provides hydroxylated polyamine derivatives, their use for the transfection of RNA polyanions into cells, and a method of transfecting cells with a polyanion, comprising mixing said polyanion with said hydroxylated polyamine derivative in a buffer and treating said cells with the mixture obtained in the previous step.