ACE2-Mimicking Liposome Composition for COVID-19 Virus Neutralization

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Solution Overview

Problem

The low availability and high dosage requirements of convalescent plasma for treating early-stage COVID-19 pose challenges, while the mechanism of action remains unclear, and there's a need for a stable, scalable alternative.

Innovation Solution

A liposome formulation containing a specific peptide sequence (22-44-G-351-357-C) attached to DSPE-PEG on its surface, composed of hydrogenated soy phosphatidylcholine, distearoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, DSPE-PEG, cholesterol, and a maleimide derivative, competes with the SARS-CoV-2 spike protein for the ACE2 receptor, immobilizing the virus and inducing antibody production.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If convalescent plasma is used for treatment, then virus neutralization and antibody-dependent cytotoxicity are achieved, but availability is very low and large doses are required

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidplasma availability

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The invention extracts and isolates the active component (ACE2 receptor peptide) from convalescent plasma, creating a purified liposomal formulation that delivers the therapeutic effect without requiring large volumes of plasma. This extracts only the essential virus-neutralizing element from the complex plasma mixture.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention creates an artificial copy of the ACE2 receptor peptide and displays it on liposome surfaces, replicating the virus-neutralization mechanism found in convalescent plasma. This synthetic peptide-liposome complex mimics and replaces the natural plasma-based therapy.

Inventive Principle:

Principle #26Copying

2Reliability

If convalescent plasma is used for treatment, then virus neutralization is achieved, but the mechanism of action remains unknown

Engineering Contradiction:

Improvevirus neutralizationVSAvoidmechanism understanding

Core Design Contradiction:

ReliabilityVSLoss of information

Solution Approach 1:

The liposomal formulation acts as an intermediary system that makes the mechanism of action visible and controllable. By displaying the ACE2 peptide on a defined liposomal carrier, the invention creates a system where the virus-binding mechanism can be studied and understood, bridging the gap between observed effectiveness and mechanistic knowledge.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Ease of manufacture

If a peptide inhibitor is developed, then virus binding inhibition is achieved, but stability during storage and in human serum is required

Engineering Contradiction:

ImprovescalabilityVSAvoidstorage stability

Core Design Contradiction:

Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The invention encapsulates the peptide within a liposomal shell composed of phospholipids and cholesterol. This flexible membrane structure protects the peptide from degradation during storage and in human serum, while maintaining the peptide's biological activity and enabling scalable manufacturing.

Inventive Principle:

Principle #30Flexible shells and thin films

Solution Approach 2:

The invention creates a composite system combining the peptide inhibitor with liposomal materials (phospholipids, cholesterol, PEG). This composite structure provides both the virus-neutralization function of the peptide and the stability, solubility, and storage properties of the liposomal carrier.

Inventive Principle:

Principle #40Composite materials

4Reliability

If plasma from recovered patients is used, then immediate virus neutralization is achieved, but risk of transmission of other diseases exists

Engineering Contradiction:

Improvevirus neutralizationVSAvoiddisease transmission risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention extracts only the virus-neutralizing ACE2 peptide component from plasma, eliminating all other plasma components that could transmit diseases. This purified peptide displayed on liposomes provides the therapeutic effect without the contamination risks of blood products.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention replaces expensive, risky plasma products with a synthetic, manufacturable peptide-liposome formulation that can be produced without using human blood, thereby eliminating the risk of transmitting blood-borne diseases while maintaining therapeutic effectiveness.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

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 liposome formulation effectively inhibits viral binding to cells, is stable for long-term storage, can be produced on an industrial scale, and avoids blood product risks, inducing antibody production.

Implementation Method 1

competes with the SARS-CoV-2 spike protein for the ACE2 receptor, immobilizing the virus

Methodology Applied

Scientific EffectCompetitive inhibition:

Implementation Method 2

immediate virus neutralization

Methodology Applied

Scientific EffectVirus neutralization:

Implementation Method 3

antibody-dependent cytotoxicity

Methodology Applied

Scientific EffectAntibody-dependent cytotoxicity:

Implementation Method 4

phagocytosis

Methodology Applied

Scientific EffectPhagocytosis:

Data Source

PatentEP4240328B1Liposome, especially for use in the treatment of covid-19

Publication Date: 2026.04.22 ACELLMED SP ZOO

Figure 1

AI summary

An object of the invention is a liposome preparation suitable for use in the treatment of COVID-19.