Propylene Glycol-Free Nanoemulsion for Stable Hydrophilic Delivery
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Solution Overview
Problem
Existing nanoemulsion formulations containing propylene glycol are prone to instability, allergic reactions, and side reactions, particularly when used with hydrophilic active agents like 5-aminolevulinic acid, leading to impurities and reduced shelf-life.
Innovation Solution
A nanoemulsion formulation without propylene glycol, comprising an aqueous phase, a lipophilic carrier, surfactant, and alcohol, with the active agent interacting with nanovesicles, ensuring less than 1% w/w propylene glycol or no propylene glycol, to enhance stability and penetration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If propylene glycol is used as a solvent and emulsifier in nanoemulsion formulations, then the formulation shows good solubility and emulsifying properties, but the formulation becomes unstable over time, generates impurities, and causes allergic reactions
Solution Approach 1:
The patent removes propylene glycol from the formulation entirely, extracting the problematic substance that causes instability and impurities while replacing its functions with alternative excipients that do not interfere with the active agent
Solution Approach 2:
The patent introduces alternative excipients as intermediary substances that can perform the solubility and emulsifying functions without the harmful effects of propylene glycol, serving as mediators between the hydrophilic active agent and the nanoemulsion system
2Reliability
If propylene glycol is used to enhance penetration and preserve the formulation, then the formulation shows improved penetration effects and preservative properties, but it causes allergic reactions and skin irritation
Solution Approach 1:
The patent extracts and eliminates propylene glycol, the substance responsible for harmful effects, while maintaining penetration enhancement through alternative mechanisms and excipients that do not cause allergic reactions
Solution Approach 2:
The patent converts the harmful presence of propylene glycol into a beneficial propylene glycol-free formulation by demonstrating that penetration enhancement can be achieved without this excipient, turning a harmful substance into a design constraint that leads to improved safety
3Quantity of substance
If propylene glycol is used as a solvent for hydrophilic compounds, then the compounds show good solubility in aqueous phase, but unwanted side reactions occur due to nucleophilic nature
Solution Approach 1:
The patent removes propylene glycol, the nucleophilic substance that causes unwanted side reactions, while maintaining the solubility of hydrophilic compounds through alternative solvents and formulation strategies that do not promote chemical reactions
Solution Approach 2:
The patent creates an inert chemical environment by eliminating propylene glycol and other nucleophilic excipients, preventing unwanted chemical reactions between the active agent and formulation components while maintaining physical stability and solubility
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 formulation maintains improved stability and penetration of the active agent, reducing impurities and allergic reactions, allowing for longer storage and effective drug release.
Implementation Method 1
Nanoemulsions are a subgroup of the emulsions that contain very fine oil in water dispersions... The dispersed droplets (liquid) or vesicles in such emulsions are composed of a lipid core surrounded by at least one surfactant or emulsifier monolayer
Implementation Method 2
Nanoemulsions are generally manufactured by mechanical fragmentation of an oily phase in an aqueous phase in the presence of a surfactant. The very small size of the oily globules is often obtained by virtue of at least one pass through a high-pressure homogenizer
Implementation Method 3
The very small size of the oily globules is often obtained by virtue of at least one pass through a high-pressure homogenizer or a sonicator
Data Source
AI summary
The present invention relates to oil in water nanoemulsions which are essentially free of propylene glycol. The nanovesicle formulations are particularly stable in regard to shelf life at different storage temperatures.