Transdermal Patch Composition for Basement Membrane Penetration
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Solution Overview
Problem
Existing transdermal delivery systems are limited in their ability to deliver a wide variety of pharmaceutical agents effectively, particularly those with higher molecular weights and lower log-p values, and often result in unwanted side effects from oral delivery.
Innovation Solution
A transdermal delivery system utilizing penetration agents, basement membrane disruptors, and vaso-modulators to facilitate the passage of active ingredients through the stratum corneum, epidermis, and basement membrane, allowing for targeted or systemic delivery with a faster onset of action.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If traditional patch technology is used for transdermal delivery, then delivery of simple compounds (high log-p, small molecular weight) is achieved, but delivery of complex pharmaceutical agents (lower log-p, higher molecular weight) is limited
Solution Approach 1:
The transdermal delivery system is divided into multiple functional layers: a stratum corneum penetration layer containing penetration enhancers, an epidermal delivery layer, and a dermal delivery layer. This segmentation allows each layer to be optimized for specific molecular weight ranges and log-p values, enabling delivery of diverse pharmaceutical agents that would be impossible with a single uniform patch structure.
Solution Approach 2:
The patent employs penetration enhancers that temporarily alter the physical and chemical parameters of skin layers, including changes in lipid fluidity, protein conformation, and membrane permeability. These parameter changes enable the skin barrier to accommodate molecules with varying molecular weights and log-p values, expanding the range of deliverable pharmaceutical agents while maintaining reliable delivery effectiveness.
2Adaptability or versatility
If oral delivery of medications is used, then a wide variety of pharmaceutical agents can be delivered, but unwanted side effects occur
Solution Approach 1:
The transdermal patch acts as an intermediary delivery system that bypasses the gastrointestinal tract and first-pass liver metabolism. By using penetration enhancers and a multi-layer structure as mediators, the system enables delivery of diverse pharmaceutical agents directly through the skin into systemic circulation, avoiding the harmful side effects associated with oral administration while maintaining the ability to deliver a wide variety of agents.
3Ease of operation
If conventional transdermal patches are used, then passive penetration through skin is achieved, but faster onset of action is not obtained
Solution Approach 1:
The patch incorporates penetration enhancers that are pre-positioned in the stratum corneum layer to temporarily disrupt the skin barrier before the active pharmaceutical ingredient needs to be delivered. This preliminary action of altering skin permeability parameters creates a window of enhanced penetration that accelerates the onset of action while maintaining the simplicity of passive transdermal application.
Solution Approach 2:
The system utilizes dynamic penetration enhancers that temporarily alter skin barrier properties during the delivery period, creating time-dependent changes in permeability. This dynamic approach allows the skin to be more permeable when needed for faster drug delivery, then return to its normal barrier function, achieving both ease of passive operation and accelerated onset of action.
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
Enables the delivery of a broader range of active pharmaceutical agents, including complex and higher molecular weight compounds, while avoiding side effects associated with oral administration and improving localized or systemic delivery efficiency.
Implementation Method 1
The penetration agent allows the basement membrane disruptor, the vaso-modulator, and the active ingredient to pass through the stratum corneum layer and the epidermis
Implementation Method 2
at least one basement membrane disruptor that reversibly denatures the basement membrane
Implementation Method 3
at least one vaso-modulator
Data Source
AI summary
The present invention relates to transdermal delivery systems, methods and kits that include an agent to penetrate the basement membrane, a membrane of the skin previously known to be difficult to penetrate. In particular, the formulation includes a basement membrane disruptor that reversibly denatures the basement membrane of the skin. The formulation of the present invention further includes having at least one penetration agent, at least one vaso-modulator, and at least one active ingredient. In an embodiment, the penetration agent includes a solvent, a lipophilic agent, a hydrophilic agent, wherein the basement membrane disruptor, the vaso-modulator, and the active ingredient pass through the stratum corneum and epidermis. The basement membrane disruptor allows the vaso-modulator and the active ingredient pass through the basement membrane to dermis. The active ingredient, once at the dermis, is delivered locally to the tissue or systemically to the blood stream.