Empty Liposomes Mimic Lipid Rafts to Inhibit Viral Entry

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Solution Overview

Problem

Current treatments for viral infections, particularly those caused by enveloped viruses like HCV and HIV, are limited in understanding the mechanisms of viral fusion and entry into host cells, and existing therapies may not effectively inhibit these processes without causing cytotoxicity.

Innovation Solution

The use of empty liposomes composed of defined lipid compositions, specifically sphingomyelin and cholesterol, which mimic cellular lipid rafts to compete with viruses for binding sites, thereby inhibiting viral entry into host cells in a dose-dependent manner without apparent cytotoxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If standard viral treatments are used to inhibit viral fusion and entry, then antiviral efficacy is improved, but cytotoxicity increases

Engineering Contradiction:
Improveantiviral efficacyVSAvoidcytotoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Empty liposomes serve as intermediary decoy structures that mimic cellular lipid rafts, intercepting viruses before they can bind to and infect host cells. The liposomes absorb viral particles through their raft-mimicking lipid composition (sphingomyelin and cholesterol), preventing viral entry into actual cells without requiring direct viral inhibition mechanisms that cause cytotoxicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates simplified copies of cellular lipid rafts in the form of empty liposomes with defined lipid compositions. These copies replicate the key functional properties of lipid rafts (high sphingomyelin and cholesterol content) to attract and bind viruses, serving as safe alternatives to actual cellular targets that would be damaged by viral infection or toxic treatments.

Inventive Principle:
Principle #26Copying

2Reliability

If cholesterol is removed from cell membranes to inhibit viral entry, then antiviral activity is improved, but membrane stability deteriorates

Engineering Contradiction:
Improveantiviral activityVSAvoidmembrane stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention extracts the essential functional components of cellular lipid rafts (sphingomyelin and cholesterol) and concentrates them into isolated empty liposome structures. By removing these components from actual cell membranes and placing them in controlled liposome formulations, the system achieves antiviral activity while preserving the stability and integrity of host cell membranes.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

Empty liposomes act as intermediary structures that sequester viral particles away from host cells. The liposomes contain high concentrations of sphingomyelin and cholesterol in a controlled environment, providing the antiviral function without requiring depletion of these essential membrane components from actual cells, thereby maintaining membrane stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If sphingomyelin is hydrolyzed to inhibit HCV entry, then antiviral effect is improved, but cell membrane integrity is compromised

Engineering Contradiction:
Improveantiviral effectVSAvoidcell membrane integrity
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention extracts sphingomyelin from cellular membranes and incorporates it into empty liposome structures. By concentrating sphingomyelin in the liposomes rather than depleting it from cells, the system achieves antiviral activity through the liposomes' raft-mimicking properties while preserving cell membrane integrity and sphingomyelin-dependent cellular functions.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

Empty liposomes create artificial copies of sphingomyelin-rich lipid raft environments that attract and bind viruses. These copies provide the necessary antiviral effect without requiring hydrolysis or depletion of sphingomyelin from actual cell membranes, maintaining cellular integrity while achieving viral inhibition.

Inventive Principle:
Principle #26Copying

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 described liposomal composition effectively reduces viral entry into host cells, demonstrating antiviral efficacy against enveloped viruses like HCV and potentially other viruses by acting as decoys for viral envelopes, offering a non-toxic and potentially broad-spectrum antiviral solution.

Implementation Method 1

empty liposomes composed of defined lipid compositions, specifically sphingomyelin and cholesterol, which mimic cellular lipid rafts to compete with viruses for binding sites

Methodology Applied
Scientific EffectMimicry of lipid raft structure:

Implementation Method 2

demonstrating antiviral efficacy against enveloped viruses like HCV and potentially other viruses by acting as decoys for viral envelopes

Methodology Applied
Scientific EffectDecoy mechanism:

Data Source

PatentUS20230028179A1Liposomes for the treatment of viral infections
Publication Date: 2023.01.26 COMBIOXIN SA
  • US20230028179A1 patent drawing

AI summary

The present invention relates to a composition comprising, preferably consisting of, (i) a single empty liposome, wherein said single empty liposome is selected from (a) an empty liposome consisting of sphingomyelin and cholesterol, wherein the amount of cholesterol is at least 20% (weight per weight); or (b) an empty liposome consisting of sphingomyelin; or (ii) a mixture of empty liposomes; wherein said mixture of empty liposomes comprises (a) a first empty liposome consisting of sphingomyelin and cholesterol, wherein the amount of cholesterol is at least 20% (weight per weight); and (b) a second empty liposome consisting of sphingomyelin; for use in a method of treating or preventing a viral infection in a mammal, preferably in a human.