Transdermal Patch Composite Matrix for Hydrophilic Drug Delivery
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Solution Overview
Problem
Current transdermal drug delivery systems face challenges in effectively delivering hydrophilic and amphiphilic drugs through the skin and into the bloodstream, as they often irritate the skin and have limited sustainability and quick onset of action.
Innovation Solution
A water- and sweat-resistant transdermal drug delivery system comprising a patch with a monolithic layer of bioadhesive polymer, film-forming agent, plasticizer, naturally occurring polysaccharide, and keratolytic agent, which provides excellent adhesive strength and sustained delivery of active agents for 8-24 hours, minimizing skin irritation and maximizing drug diffusion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If current transdermal delivery devices are used to deliver lipophilic small molecule drugs, then delivery is successful, but it remains difficult to transdermally deliver hydrophilic drugs through the skin and into the bloodstream
Solution Approach 1:
The patent employs a composite adhesive matrix comprising both lipophilic and hydrophilic components, allowing the system to deliver both lipophilic and hydrophilic drugs effectively. The lipophilic adhesive component facilitates delivery of lipophilic drugs, while the hydrophilic component enables delivery of hydrophilic drugs, thus achieving versatility across different drug types without compromising delivery effectiveness.
Solution Approach 2:
The patent modifies the chemical and physical parameters of the adhesive matrix by incorporating multiple components with different properties (lipophilic and hydrophilic). This parameter change allows the adhesive to interact with and deliver different types of drugs (lipophilic, hydrophilic, and amphiphilic) effectively, resolving the limitation of current devices that are optimized for only lipophilic small molecules.
2Ease of operation
If transdermal drug delivery is used to bypass liver metabolism, then patient compliance improves, but only a limited number of drugs are amenable to transdermal administration
Solution Approach 1:
The composite adhesive matrix with both lipophilic and hydrophilic components expands the range of drugs suitable for transdermal delivery. This allows more drugs (including hydrophilic, lipophilic, and amphiphilic types) to be administered transdermally, maintaining patient compliance benefits while increasing drug applicability.
Solution Approach 2:
The adhesive system is designed to be universal, capable of delivering multiple types of drugs (lipophilic, hydrophilic, and amphiphilic) through a single platform. This multi-functionality allows the transdermal system to bypass liver metabolism for a broader range of drugs, improving both patient compliance and drug applicability.
3Area of stationary object
If a small patch size is used to minimize skin surface area, then less skin is required for administration, but the amount of active agent that can be delivered is limited
Solution Approach 1:
The composite adhesive matrix increases the drug loading capacity per unit area by incorporating multiple components that can accommodate different types of drugs. This allows a small patch to deliver larger amounts of active agents compared to conventional single-component adhesives, as the composite structure can hold and release higher concentrations of both lipophilic and hydrophilic drugs.
Solution Approach 2:
The patent changes the concentration and composition parameters of the adhesive matrix to optimize drug loading capacity. By adjusting the ratios of lipophilic and hydrophilic components and incorporating penetration enhancers, the system achieves higher active agent amounts in a compact patch size, resolving the trade-off between patch area and drug quantity.
4Speed
If quick onset of action is achieved within 15 minutes, then rapid drug delivery is accomplished, but sustained delivery for 8-24 hours becomes challenging
Solution Approach 1:
The composite adhesive matrix with both lipophilic and hydrophilic components enables simultaneous rapid penetration and sustained release. The lipophilic component facilitates quick penetration through the stratum corneum for rapid onset, while the hydrophilic component provides a reservoir for sustained release over 8-24 hours, resolving the contradiction between speed and duration.
Solution Approach 2:
The system employs a two-phase delivery mechanism: an initial rapid release phase for quick onset of action, followed by a sustained release phase for prolonged effectiveness. This periodic action pattern allows the patch to achieve both quick onset within 15 minutes and sustained delivery for 8-24 hours through controlled release kinetics.
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 system achieves quick onset of action within 15 minutes, delivers 65-100% of active agents into the skin within 8-24 hours, and is suitable for sensitive skin populations, improving patient compliance and reducing side effects.
Implementation Method 1
10-50% (w/w) of a keratolytic agent
Implementation Method 2
10-30% (w/w) of a bioadhesive polymer
Implementation Method 3
delivers 65-100% of active agents into the skin within 8-24 hours
Data Source
AI summary
Provided herein is a water- and sweat-resistant transdermal drug delivery system for application to the skin of a mammal that comprises a patch having a diameter between 1 and 8 cm in length and a surface area between 4 and 8 cm2. Also provided are methods of producing the transdermal drug delivery system and methods of treatment comprising the use of the transdermal drug delivery system.