Polymer-Free Microstructure Array for Transdermal Protein Delivery
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Solution Overview
Problem
Current methods for delivering therapeutic proteins and biomolecules, such as those for cancer and autoimmune disease treatment, face challenges due to their large and complex nature, requiring repeated administration and facing issues like gastrointestinal degradation and low bioavailability through traditional routes, while transdermal delivery systems have limitations in penetrating the skin effectively.
Innovation Solution
A microstructure array comprising a biodegradable distal layer with a therapeutic macromolecule and a stabilizing excipient, such as sucrose or trehalose, that provides mechanical strength for transdermal administration, allowing for the delivery of large biomolecules like proteins and antibodies through the skin without the need for structural polymers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If structural polymers are used in microneedle arrays to provide mechanical strength, then the microstructures can penetrate skin effectively, but the complexity of the device increases and manufacturing becomes more difficult
Solution Approach 1:
The patent removes structural polymers from the microneedle composition entirely. Instead of using polymer matrices to provide mechanical strength, the invention uses only the therapeutic macromolecule itself, which forms the structural framework through its own molecular properties. This extraction of the structural polymer component simplifies the device composition and manufacturing while maintaining the necessary mechanical strength for skin penetration.
Solution Approach 2:
The therapeutic macromolecule serves dual functions simultaneously: it provides both the therapeutic effect and the structural framework. The macromolecule's own molecular structure gives rise to the mechanical properties needed for penetration, eliminating the need for separate structural components. This self-service approach reduces device complexity while maintaining functionality.
2Ease of manufacture
If traditional administration routes are used for therapeutic proteins, then the delivery process is simple, but the proteins face gastrointestinal degradation and low bioavailability
Solution Approach 1:
The microneedle array acts as an intermediary delivery system that bridges the gap between simple administration and reliable protein delivery. The microneedles penetrate the skin barrier to deliver proteins directly to subcutaneous tissues, avoiding gastrointestinal degradation while maintaining ease of use. The excipient matrix facilitates this by enabling simple application while ensuring reliable protein delivery through controlled release.
Solution Approach 2:
The invention changes the delivery parameter from oral/gastrointestinal route to transdermal route. This parameter change in the administration pathway eliminates gastrointestinal degradation while maintaining ease of use. The microneedle system transforms the delivery parameter to achieve both simplicity and reliability simultaneously.
3Reliability
If transdermal delivery systems are used to penetrate skin, then protein bioavailability improves, but the ability to penetrate the skin barrier effectively is limited
Solution Approach 1:
The invention changes the physical-chemical parameters of the microneedle composition by using only therapeutic macromolecule and excipient without structural polymers. This parameter change creates microneedles that maintain sufficient mechanical strength for penetration while enabling effective protein delivery. The excipient matrix parameters are optimized to balance penetration capability with bioavailability.
Solution Approach 2:
The microneedle uses a composite structure of therapeutic macromolecule and excipient that works synergistically. The macromolecule provides structural framework while the excipient provides matrix for drug delivery and stability. This composite material approach achieves both effective penetration and reliable protein delivery, overcoming the limitations of traditional transdermal systems.
4Reliability
If repeated administration is used for therapeutic proteins, then the treatment effectiveness is maintained, but the loss of time increases
Solution Approach 1:
The microneedle array provides dynamic, sustained release of the therapeutic protein over time. The excipient matrix controls the release kinetics to maintain effective protein levels in the subcutaneous tissue for extended periods. This dynamic release mechanism reduces the need for repeated administrations, thereby reducing time loss while maintaining treatment effectiveness.
Solution Approach 2:
The microneedle system enables continuous or extended-term protein delivery through controlled release from the excipient matrix. This continuity of useful action eliminates the need for repeated administrations to maintain treatment effectiveness, reducing the cumulative time loss associated with multiple administration sessions.
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 microstructure array enables efficient transdermal delivery of therapeutic macromolecules, maintaining stability and bioavailability, and overcoming the limitations of traditional administration routes by providing mechanical strength sufficient for skin penetration and extended release into subcutaneous layers.
Implementation Method 1
The distal layer comprises at least one drug and a stabilizing excipient
Implementation Method 2
each of the plurality of microstructures has mechanical strength sufficient to provide transdermal administration to a subject
Implementation Method 3
The microstructure comprises a backing having a first surface and a second surface opposed thereto, and a microstructure array comprising the plurality of microstructures, wherein the plurality of microstructures extend outwardly from the first surface of the backing. Each of the plurality of microstructures comprises a biodegradable distal layer
Data Source
AI summary
A microprojection array comprising an approximately planar base and a plurality of microprojections, wherein the array comprises a therapeutic macromolecule and a stabilizing excipient. Described herein are microstructures having a proximal and distal layer, wherein the distal layer which contains the therapeutic molecule does not rely on the presence of a structure-forming polymer to impart the mechanical strength necessary to penetrate the skin. Methods of forming the array, and methods of using the array are contemplated.