Formulation for transdermal delivery
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Solution Overview
Problem
Existing transdermal microemulsions face challenges in maintaining stability across a wide range of organic to aqueous ratios, which affects their ability to effectively deliver drugs through the skin, while also requiring components that meet regulatory approval and avoid evaporation.
Innovation Solution
An organic composition comprising fatty alcohol or ester, ethoxylated castor oil, and specific cosolvents forms stable water-in-oil microemulsions across a broad range of water contents, using components approved for medical use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If a microemulsion uses light organic components that blend well with water, then the microemulsion forms stable emulsions, but the organic components evaporate quickly and the microemulsion cannot remain on the skin during drug absorption
Solution Approach 1:
The patent changes the molecular weight parameter of the organic components, transitioning from light organic solvents to heavier organic esters and hydrocarbons with higher boiling points. This parameter change reduces evaporation while maintaining microemulsion stability through the balanced composition of multiple organic components including esters like isopropyl myristate and hydrocarbons like isododecane.
2Stability of the object's composition
If a microemulsion uses a narrow range of organic to aqueous ratios, then the microemulsion remains stable, but it cannot be formulated effectively for a wide variety of drugs with different solubility requirements
Solution Approach 1:
The patent creates a universal organic composition system that can accommodate multiple drugs with different solubility characteristics. The multi-component organic phase including esters, hydrocarbons, and ethoxylated castor oil provides a versatile solvent system that can dissolve both lipophilic and moderately hydrophilic drugs while maintaining microemulsion stability across various water content levels.
Solution Approach 2:
The patent uses a composite organic composition combining multiple components (esters, hydrocarbons, ethoxylated castor oil) rather than a single organic solvent. This composite approach allows the system to achieve both stability and versatility, as each component contributes different properties that collectively enable broad drug formulation capability.
3Productivity
If a microemulsion contains high concentrations of drug and penetration enhancers, then the drug delivery effectiveness increases, but the microemulsion may separate into oil and water phases
Solution Approach 1:
The patent adjusts the composition parameters by incorporating specific ratios of organic components including esters, hydrocarbons, and ethoxylated castor oil. These compositional changes enhance the microemulsion's capacity to accommodate high drug and penetration enhancer concentrations while maintaining phase stability through the balanced amphiphilic character of the organic phase.
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 solution enables the formation of stable microemulsions capable of delivering drugs effectively through the skin over an extended period, maintaining stability and regulatory compliance.
Implementation Method 1
The formulation is absorbed through the skin by osmosis and carries the dissolved drugs with it.
Implementation Method 2
an organic composition that contains fatty alcohol or ester, ethoxylated castor oil and specific cosolvents can maintain a stable water-in-oil microemulsion across a relatively wide range of water-to-organic ratios
Data Source
AI summary
Stable microemulsions that can contain a broad range of water content can be made using an organic mixture that contains: a) from 5 to 60 weight percent of a fatty alcohol or fatty ester; b) from 14 to 40 weight percent of ethoxylated castor oil; and c) from 20 to 65 weight percent of a cosolvent selected from the group consisting of lower alkyl diethylene glycol ether, lower alkyl triethylene glycol ether and propylene glycol diacetate; and d) from 5 to 25 weight percent of a chemical penetration enhancer for skin.