Polycationic-Polyanionic Complex for Peptide Delivery

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Solution Overview

Problem

Current peptide/protein delivery methods into eukaryotic cells are inefficient, prone to protein denaturation and degradation, and limited by the type of target protein, molecular weight, or cell type, lacking a universal and robust solution.

Innovation Solution

A composition comprising a polycationic agent and a polyanionic agent, where the polyanionic agent is an inorganic polyphosphate or polyoxometalate, forming ionic complexes that enhance peptide/protein delivery efficiency across a wide range of proteins and cell types, without the need for covalent coupling agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If current peptide/protein delivery methods are used, then delivery can be achieved, but delivery efficiency is low and protein denaturation and degradation occur

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidprotein integrity
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent uses a composite delivery system combining cationic lipids with cell-penetrating peptides to create a synergistic effect. The cationic lipids form complexes with the protein while the peptides facilitate cellular uptake, achieving both high delivery efficiency and protein protection through the combined properties of different materials

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent introduces delivery agents as intermediaries between the protein and cell. These agents (cationic lipids and peptides) mediate the interaction by forming protective complexes that shield the protein from degradation while enabling efficient cellular uptake through membrane interaction

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If delivery agents are used to facilitate protein delivery, then delivery into cells is improved, but the method is limited by target protein type, molecular weight, or cell type

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidapplicability across different proteins and cell types
Core Design Contradiction:
ProductivityVSAdaptability or versatility

Solution Approach 1:

The patent employs cell-penetrating peptides with universal transduction domains that can deliver various proteins across different cell types. The peptides are designed to function broadly rather than being specific to particular proteins or cell types, enhancing the versatility of the delivery system

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

3Productivity

If conventional transfection agents are used, then protein delivery is facilitated, but the agents may be toxic to host cells

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidcell toxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the charge ratio and composition of the delivery complex to achieve effective delivery while minimizing toxicity. By adjusting parameters such as the lipid-to-protein ratio and peptide concentration, the system maintains delivery efficiency while reducing harmful effects on host cells

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 solution achieves more efficient, uniform, and robust peptide/protein delivery, increasing transfection efficiency and maintaining protein integrity, as demonstrated by higher mean fluorescence intensity and cytosolic localization of delivered proteins.

Implementation Method 1

A composition for delivering a peptide or protein into a cell, which composition comprises a polycationic agent and a polyanionic agent

Methodology Applied
Scientific EffectIonic bonding: Electrostatics

Data Source

PatentUS9856456B2Delivery agent
Publication Date: 2018.01.02 THERMO FISHER SCI BALTICS UAB
  • US9856456B2 patent drawing
  • US9856456B2 patent drawing
  • US9856456B2 patent drawing

AI summary

A composition comprising a polycationic agent and a polyanionic agent, and kits comprising the composition, is provided. In embodiments, the polyanionic agent is a nucleic acid and the polycationic agent is a modified polyalkyleneimine polymer.