Ivermectin Sustained Release Copolymer Matrix for Prophylaxis

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Solution Overview

Problem

Current methods lack effective prophylactic treatments for COVID-19, particularly for vulnerable populations at high risk of SARS-CoV-2 exposure or infection, with existing treatments showing limited efficacy in preventing viral replication and clinical benefits.

Innovation Solution

A method involving the administration of ivermectin in a sustained release formulation, incorporated into a diblock/triblock copolymer matrix, to inhibit SARS-CoV-2 replication in vulnerable individuals, providing prolonged protection against COVID-19 through subcutaneous injection with a frequency of no more than once every 21 days.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If ivermectin is administered as a single dose, then the treatment is simple and safe, but it does not provide prolonged protection and requires frequent re-administration

Engineering Contradiction:
ImproveDuration of antiviral protectionVSAvoidFormulation complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent changes the physical and chemical parameters of ivermectin by incorporating it into a sustained-release formulation with specific polymers (PLGA, PEG-PLA) and controlled particle size (10-500 micrometers), transforming it from a rapidly cleared single-dose medication into a formulation that maintains therapeutic levels for at least 21 days

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite material system consisting of ivermectin combined with biodegradable polymers (PLGA and/or PEG-PLA) in specific ratios, forming a sustained-release formulation that provides prolonged antiviral protection while maintaining safety and efficacy

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If ivermectin is administered frequently to maintain protection, then prolonged protection is achieved, but the treatment burden and risk of side effects increase

Engineering Contradiction:
ImproveDuration of antiviral protectionVSAvoidSide effects and treatment burden
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent establishes a periodic dosing regimen where the sustained-release formulation is administered once every 21 days or longer, transforming the treatment from frequent single-dose administration to a manageable periodic schedule that maintains protection while reducing treatment burden and side effect risk

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The sustained-release formulation provides self-service by automatically maintaining therapeutic ivermectin levels in the body for at least 21 days without requiring frequent patient intervention, thereby reducing treatment burden while ensuring continuous protection

Inventive Principle:
Principle #25Self-service

3Reliability

If high dose ivermectin is administered to ensure efficacy, then viral replication is effectively inhibited, but safety concerns and side effects increase

Engineering Contradiction:
ImproveEfficacy in inhibiting viral replicationVSAvoidSafety and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs preliminary action by administering ivermectin in advance (prophylactically) before SARS-CoV-2 infection occurs or within 72 hours of exposure, allowing the sustained-release formulation to establish therapeutic levels before viral replication begins, thereby ensuring efficacy at lower, safer doses

Inventive Principle:
Principle #10Preliminary action

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 ivermectin formulation effectively inhibits SARS-CoV-2 replication, offering prolonged protection for at least 21 days, reducing the severity of COVID-19 symptoms and preventing development of the disease in exposed individuals, with a suitable dose and low injection volume for ease of administration.

Implementation Method 1

the ivermectin may be in the form of a sustained release formulation comprising a triblock copolymer and a diblock copolymer

Methodology Applied
Scientific EffectSustained release:

Implementation Method 2

a biodegradable triblock copolymer having the formula: poly(lactic acid)v-poly(ethylene glycol)w-poly(lactic acid)x

Methodology Applied
Scientific EffectControlled degradation:

Data Source

PatentUS20240099964A1Methods and Compositions for the Prophylactic Treatment of SARS-CoV-2 virus (COVID-19)
Publication Date: 2024.03.28 MEDINCELL SA
  • US20240099964A1 patent drawing
  • US20240099964A1 patent drawing
  • US20240099964A1 patent drawing

AI summary

A method of prophylactically treating COVID-19 in subject who is at high risk for exposure to SARS-CoV-2 virus or who is been recently exposed to SARS-CoV-2, but who tests negative for the virus, by administering to said subject an effective dose of ivermectin to inhibit one or symptoms of SARS-CoV-2 virus.