Hydrotrope-Modified Active Agents for Mucosal Delivery
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Solution Overview
Problem
Mucosal membranes pose a barrier to the effective delivery of active agents due to their structure and chemical properties, limiting the passive transport of both hydrophilic and lipophilic compounds, with current methods often increasing solubility at the expense of permeability.
Innovation Solution
A pharmaceutical composition comprising hydrotropes in less than 15% by weight, combined with active agents having a partition coefficient (log P or log D) between 0 and 5, enhances penetration through mucosal membranes by modifying the lipophilicity of the active agents, allowing them to bypass lipid-rich cellular membranes and intercellular lipids without increasing solubility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional methods are used to increase solubility of active agents, then solubility is improved, but permeability through mucosal membranes deteriorates
Solution Approach 1:
The patent modifies the lipophilicity parameter of active agents by combining them with hydrotropes, changing the partition coefficient (log P or log D) to an optimal range between 0 and 5. This parameter change enables the active agents to achieve both adequate solubility and enhanced permeability through mucosal membranes, resolving the contradiction between solubility improvement and permeability maintenance.
Solution Approach 2:
The patent creates a composite system by combining active agents with hydrotropes in specific ratios. This composite approach allows the mixture to exhibit properties that neither component has alone - the hydrotropes enhance the lipophilicity and membrane permeability of the active agents while maintaining adequate solubility, thus resolving the solubility-permeability contradiction.
2Ease of operation
If passive transport is attempted through mucosal membranes, then simplicity of delivery is improved, but transport efficiency deteriorates due to membrane barriers
Solution Approach 1:
The patent changes the physicochemical parameters of the active agents, specifically adjusting the partition coefficient to between 0 and 5 through combination with hydrotropes. This modification enables the agents to effectively traverse the complex mucosal membrane structure through passive transport, maintaining simplicity while dramatically improving transport efficiency.
3Quantity of substance
If active agents interact with intercellular lipids and cell membranes, then initial partitioning into mucosal tissue is improved, but overall penetration deteriorates due to binding
Solution Approach 1:
The patent optimizes the partition coefficient (log P or log D) of active agents to a specific range between 0 and 5 through hydrotrope combination. This balanced parameter setting allows sufficient partitioning into the lipid-rich intercellular spaces while preventing excessive binding that would trap the agents, thereby achieving both good tissue partitioning and effective penetration through the mucosal barrier.
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 approach increases the flux of active agents through mucosal membranes, improving bioavailability by reducing binding to lipids and proteins, while maintaining or enhancing permeability without the need for high concentration gradients.
Implementation Method 1
enhances penetration through mucosal membranes by modifying the lipophilicity of the active agents, allowing them to bypass lipid-rich cellular membranes and intercellular lipids
Implementation Method 2
increases the flux of active agents through mucosal membranes, improving bioavailability by reducing binding to lipids and proteins
Data Source
AI summary
A method to increase the penetration of active agents through mucosal membranes, the method comprising the step of: a) administering to a subject in need a composition comprising: i) one or more hydrotropes in a total amount of less than 15% by weight of the composition; and ii) an active agent with a partition co-efficient (log P) or distribution coefficient (log D) of between 0 and 5.