Lactoferrin Inhibits SARS-CoV-2 Viral Entry via Heparin Binding

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Solution Overview

Problem

Current treatments for COVID-19 lack effective solutions for preventing and treating SARS-CoV-2 viral entry and associated symptoms, with a need for rapidly deployable interventions to reduce morbidity and mortality.

Innovation Solution

Pharmaceutical compositions comprising lactoferrin, either naturally occurring or recombinant, in oral or intravenous formulations, alone or combined with agents like remdesivir, hydroxychloroquine, and dexamethasone, which inhibit SARS-CoV-2 viral entry and alleviate symptoms by enhancing immune response and reducing pro-inflammatory cytokines.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for COVID-19 are used, then some symptoms may be managed, but effective prevention and treatment of SARS-CoV-2 viral entry is lacking

Engineering Contradiction:

Improveefficacy in preventing viral entryVSAvoidlack of effective solutions

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

Lactoferrin acts as an intermediary substance that binds to heparin sulfate proteoglycans on the cell surface, blocking the viral entry mechanism. This mediator approach prevents SARS-CoV-2 from attaching to and entering host cells, directly addressing the lack of effective prevention treatments.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the parameter of viral entry inhibition by introducing lactoferrin, which fundamentally alters the interaction between the virus and host cells. This parameter change transforms the ineffective current treatment state into an effective prevention state.

Inventive Principle:

Principle #35Parameter changes

2Ease of operation

If lactoferrin is administered orally, then gastrointestinal symptoms are mitigated and viral entry is prevented, but the need for multiple administration routes exists

Engineering Contradiction:

Improveoral availabilityVSAvoidadministration routes

Core Design Contradiction:

Ease of operationVSAdaptability or versatility

Solution Approach 1:

Lactoferrin is designed with multi-functionality, serving both as an antiviral agent preventing SARS-CoV-2 entry and as a gastrointestinal protective agent. This universal substance addresses multiple needs through a single compound, reducing the requirement for multiple different medications.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The oral formulation of lactoferrin serves the dual purpose of treating gastrointestinal symptoms and preventing viral entry simultaneously. The same substance that protects the GI tract also provides systemic antiviral protection, allowing the treatment to serve itself across multiple functions.

Inventive Principle:

Principle #25Self-service

3Reliability

If lactoferrin combinations are used, then anti-viral activity is enhanced, but treatment complexity increases

Engineering Contradiction:

Improveanti-viral activityVSAvoidtreatment regimen

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The invention merges lactoferrin with other antiviral agents in combination formulations, creating a synergistic effect that enhances anti-viral activity. By combining substances that work through complementary mechanisms, the treatment achieves greater reliability in preventing viral entry and managing symptoms.

Inventive Principle:

Principle #5Merging (Combining)

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

Lactoferrin demonstrates nearly 100% efficacy in preventing SARS-CoV-2 infection and significantly reduces viral replication, with combinations showing enhanced anti-viral activity, effectively treating symptoms such as fever, fatigue, and respiratory distress.

Implementation Method 1

blocks SARS-CoV-2 entry through binding to heparin sulfate proteoglycans

Methodology Applied

Scientific EffectBinding: Adsorption

Data Source

PatentUS20230149515A1Inhibition of SARS-cov-2 viral entry through oral administration of lactoferrin and uses thereof

Publication Date: 2023.05.18 THE RGT UNIV OF MICHIGAN

AI summary

This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical compositions comprising lactoferrin (e.g., naturally occurring lactoferrin, recombinant lactoferrin) which function as inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral entry into a subject (e.g., human subject). The invention further relates to methods of preventing, treating and/or ameliorating symptoms related to conditions caused by the SARS-CoV-2 virus (e.g., COVID-19), comprising administering to a subject (e.g., human subject) lactoferrin (e.g., naturally occurring lactoferrin, recombinant lactoferrin) (e.g., oral formulation of lactoferrin, intravenous (IV) formulation of lactoferrin) alone or with additional agents (e.g., remdesivir).