Reverse Microemulsion Transdermal Delivery of Hydrophilic Agents
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current transdermal delivery methods face challenges in effectively delivering hydrophilic biologically-active agents through the skin due to their insolubility in traditional hydrophobic solvents, leading to inefficiencies and discomfort during application.
Innovation Solution
A composition using a reverse microemulsion system with a hydrophobic, volatile solvent and a reverse emulsion surfactant solubilizes hydrophilic agents, allowing for non-stinging, painless penetration through the skin, utilizing hexamethyldisiloxane as a solvent and sodium bis(2-ethylhexyl)sulfosuccinate as a surfactant to form a stable, clear solution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If hydrophilic biologically-active agents are delivered using traditional hydrophobic solvents, then transdermal delivery can be achieved, but the agents are insoluble in the solvents leading to delivery inefficiency
Solution Approach 1:
The patent uses reverse emulsion surfactants as intermediary substances that enable hydrophilic biologically-active agents to be solubilized in hydrophobic volatile solvents. The surfactant forms a bridge between the polar agent and nonpolar solvent, creating a stable reverse microemulsion system that resolves the solubility contradiction while maintaining transdermal delivery capability.
Solution Approach 2:
The patent changes the physical-chemical parameters of the delivery system by using reverse microemulsions with specific HLB values (3-11) and controlling the water content (0-10 wt%) to achieve optimal solubility of hydrophilic agents in hydrophobic solvents. This parameter optimization enables both solubility and transdermal penetration.
2Ease of operation
If volatile hydrophobic solvents are used for transdermal delivery, then rapid evaporation and non-stinging application are achieved, but hydrophilic agents cannot be solubilized
Solution Approach 1:
Reverse emulsion surfactants serve as mediators that allow hydrophilic agents to be incorporated into volatile hydrophobic solvent systems without compromising application comfort. The surfactant enables solubilization while the volatile solvent maintains rapid evaporation and non-stinging properties.
Solution Approach 2:
The patent creates a composite delivery system combining volatile hydrophobic solvent, reverse emulsion surfactant, and hydrophilic biologically-active agent. This composite formulation achieves both solubility of polar agents and the desirable application characteristics of volatile hydrophobic solvents.
3Reliability
If reverse microemulsion is used to solubilize hydrophilic agents, then solubility is improved, but the system complexity increases
Solution Approach 1:
The patent simplifies the reverse microemulsion system by optimizing key parameters: using surfactants with HLB values of 3-11, limiting water content to 0-10 wt%, and selecting volatile solvents with specific properties. These parameter constraints reduce formulation complexity while maintaining solubility effectiveness.
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
This method enables efficient, rapid, and sustained transdermal delivery of hydrophilic agents, overcoming solubility issues and providing a conformal coating that maintains efficacy and comfort during application and healing.
Implementation Method 1
hydrophilic, polar, biologically active agents that are solubilized by a reverse emulsion surfactant into a microemulsion
Implementation Method 2
solubilizing them in a reverse microemulsion
Implementation Method 3
penetrating the stratum corneum of the skin
Implementation Method 4
Transdermal delivery is augmented by the addition of a penetration enhancer
Implementation Method 5
volatile, hydrophobic solvent... after solvent evaporation
Data Source
AI summary
A composition and method adapted for delivery of hydrophilic, biologically-active agents are disclosed. The composition can include a reverse microemulsion formed from at least one hydrophilic, biologically-active agent solubilized by a hydrophobic reverse emulsion surfactant in a non-stinging, volatile, hydrophobic solvent. The non-stinging, volatile, hydrophobic solvent is selected from the group consisting of volatile linear and cyclic siloxanes, volatile linear, branched, and cyclic alkanes, volatile fluorocarbons and chlorofluorocarbons, liquid carbon dioxide under pressure, and combinations thereof. The reverse microemulsion can be an optically clear solution.