Poloxamer Compositions with Hydrophobic Vicinal Diols
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Solution Overview
Problem
Topically applied formulations have a short duration of action due to limited residence time on biological surfaces, making it challenging to maintain active agents at the target site for effective treatment.
Innovation Solution
The addition of hydrophobic vicinal diols, such as monoalkyl glycols, monoalkyl glycerols, and monoacyl glycerols, to aqueous poloxamer compositions lowers the sol-gel temperature, increasing viscosity and residence time on biological surfaces.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Temperature
If hydrophobic vicinal diols are added to aqueous poloxamer compositions, then the sol-gel temperature decreases and viscosity increases, but the formulation complexity increases
Solution Approach 1:
The patent applies parameter changes by adding hydrophobic vicinal diols (specific compounds with defined chemical structures) to modify the sol-gel transition temperature parameter of poloxamer compositions. This chemical additive changes the physical parameters (temperature and viscosity) of the formulation in a controlled manner, resolving the contradiction between achieving desired temperature reduction and maintaining formulation simplicity.
2Duration of action of moving object
If poloxamer concentration is increased to maintain gel structure, then the residence time on biological surfaces increases, but the sol-gel transition temperature increases
Solution Approach 1:
The patent uses parameter changes by introducing hydrophobic vicinal diols that allow the sol-gel transition temperature to be lowered while maintaining adequate gel structure. This enables the formulation to achieve both extended residence time (through gel properties) and reduced transition temperature, resolving the contradiction between these two parameters.
Solution Approach 2:
The patent creates a composite material system by combining poloxamer with hydrophobic vicinal diols. This composite approach allows the formulation to exhibit modified rheological properties where the diol components work synergistically with poloxamer to achieve both gel stability and lower transition temperature, resolving the contradiction between residence time and transition temperature.
3Stability of the object's composition
If excipients that increase sol-gel transition temperature are used (such as hydrochloric acid, propylene glycol, ethanol), then the gel structure is stabilized, but the residence time on biological surfaces decreases
Solution Approach 1:
The patent applies inversion by using excipients (hydrophobic vicinal diols) that have the opposite effect of conventional stabilizing excipients. Instead of increasing the sol-gel transition temperature to stabilize the gel, the patent uses diols that decrease the transition temperature while still maintaining gel structure through different mechanisms, thereby resolving the contradiction between gel stability and residence time.
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 decreased sol-gel temperature allows for a higher composition viscosity, enabling active agents to remain in proximity to biological surfaces for an extended period, enhancing the effectiveness of topical treatments.
Implementation Method 1
Poloxamers are triblock copolymers of poly(ethylene oxide) and poly(propylene oxide) that have thermoreversible properties wherein they transform from a liquid-like behavior to gel-like behavior above a certain temperature and certain percent composition in aqueous systems. This phenomenon is termed the sol-gel transition, most often represented by the sol-gel transition temperature, Tsol-gel.
Data Source
AI summary
The reduction in the sol-gel temperature of aqueous poloxamer surfactant compositions by the addition of hydrophobic vicinal diols is provided. Lowering of the sol-gel temperature and the gelling efficiency of water-soluble poloxamer block copolymers of polyethylene oxide-b-polypropylene oxide-b-polyethylene oxide has been markedly improved by the addition of small amounts of at least one hydrophobic vicinal diol, such as monoalkyl glycols, monoalkyl glycerols, or monoacyl glycerols. The decrease in the sol-gel temperature facilitates gel formation, and such gels exhibit greater residence time on a surface, particularly those with biological properties.