PMD Antiviral Formulation Stability and Sprayability
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Solution Overview
Problem
Current antiviral formulations containing p-Menthane-3,8-diol (PMD) face challenges in stability and sprayability, particularly at lower concentrations, which affects their effectiveness and practical application as antiviral agents, due to crystallization issues that interfere with delivery mechanisms.
Innovation Solution
Development of stable, sprayable antiviral compositions comprising 0.1-25% PMD with specific solvents, emulsifiers, and surfactants, such as short-chain alcohols and non-ionic ethoxylated sorbitan esters, to prevent crystallization and ensure effective delivery, along with the option of incorporating these compositions into non-sprayable preparations like creams or lotions for topical application.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If PMD is used at lower concentrations in antiviral formulations, then the formulation becomes more suitable for antiviral use with reduced side effects, but PMD crystallizes which interferes with spray delivery mechanisms
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by introducing specific co-solvents (ethylene glycol, propylene glycol) and surfactants (polysorbate 80, glyceryl oleate citrate) that modify the solubility characteristics of PMD. These parameter changes allow PMD to remain in solution at lower concentrations (0.1-25% w/v) without crystallizing, thereby maintaining sprayability while achieving effective antiviral concentrations
Solution Approach 2:
The patent creates a composite formulation system combining PMD with multiple auxiliary substances including co-solvents, emulsifiers, and surfactants. This composite approach ensures that PMD remains soluble and stable in the formulation matrix, preventing crystallization issues that would otherwise occur at lower concentrations and interfere with spray delivery mechanisms
2Strength
If PMD concentration is increased to improve antiviral activity, then viral envelope disruption is enhanced, but the formulation becomes less stable and more prone to crystallization
Solution Approach 1:
The patent modifies the formulation parameters by incorporating specific co-solvents and surfactants that expand the stable concentration range of PMD. These additives change the solubility product and crystallization temperature of PMD in the formulation, allowing higher concentrations to be maintained in solution without precipitating, thus enhancing antiviral activity while preserving formulation stability
Solution Approach 2:
The patent introduces intermediary substances (co-solvents like ethylene glycol and propylene glycol, and surfactants like polysorbate 80) that act as mediators between PMD and the aqueous formulation base. These intermediaries facilitate the solubilization of PMD at higher concentrations, preventing direct interaction between PMD molecules that would lead to crystallization, thereby maintaining both stability and enhanced antiviral strength
3Quantity of substance
If conventional insect repellent formulations are repurposed as antiviral agents, then PMD content is sufficient for insect repellency, but the formulations are inappropriate for antiviral use due to stability and application issues
Solution Approach 1:
The patent adjusts the formulation parameters by reducing PMD concentration to the antiviral-effective range (0.1-25% w/v) while compensating with co-solvents and surfactants that prevent crystallization. This parameter modification transforms the formulation from an insect repellent optimized for high PMD content to an antiviral formulation optimized for stability and sprayability at lower, more appropriate PMD concentrations
Solution Approach 2:
The patent segments the formulation into distinct functional components: PMD as the antiviral active ingredient, co-solvents for solubility enhancement, surfactants for stabilization, and water as the base. This segmentation allows each component to be optimized for its specific function, enabling the formulation to achieve antiviral effectiveness without the stability and application problems of conventional high-concentration insect repellent formulations
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 compositions maintain stability and effectiveness, providing broad-spectrum antiviral, bactericidal, and fungicidal properties, with enhanced shelf life and ease of application, demonstrated by significant reductions in viral and bacterial loads, including coronaviruses and skin pathogens.
Implementation Method 1
since all these viruses have a lipid envelope, the compositions may also be effective against other viruses having a lipid envelope, including coronaviruses
Implementation Method 2
PMD showed a tendency to crystallise, in particular when used at concentrations lower than those which may be found in conventional insect repellents, such that potential formulations required to be modified in order to reduce crystallisation
Data Source
AI summary
Described herein are compositions including p-Menthane-3,8-diol (PMD) having antiviral properties. The compositions are formulated to be stable and sprayable. Other formulations may be formulated as a topical barrier preparation.