Glycerol-Silicone Elastomer Zero-Order Release
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Solution Overview
Problem
Current drug delivery systems face challenges in achieving controlled and sustained release of active substances, particularly in achieving zero-order release profiles, which are technologically difficult to create and often result in higher costs, and are prone to an initial burst effect due to Fickian transport.
Innovation Solution
The development of elastomeric silicone compositions with multiple distinct glycerol phases embedded in a silicone matrix, where the glycerol phases can be tuned for zero- or near-zero-order release kinetics by adjusting glycerol content, domain size, and membrane thickness, allowing for controlled release of active substances without an initial burst.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If simple polymer-based active substance delivery systems with uniform dispersion are used, then ease of manufacture is improved, but release precision deteriorates due to burst effect and inability to achieve zero-order release
Solution Approach 1:
The invention segments the active substance into discrete domains within the polymer matrix, separating the release mechanism from simple uniform dispersion. This segmentation allows controlled release kinetics by managing the interfaces between domains and matrix, eliminating burst effect while maintaining manufacturability
Solution Approach 2:
The invention creates local quality variations within the polymer matrix by incorporating domains with different properties (different active substances, different concentrations, or different polymer compositions). This local differentiation enables precise control over release rates and kinetics, achieving zero-order release profiles
2Manufacturing precision
If sophisticated systems based on different polymers are designed to modify release profiles, then release precision is improved, but device complexity and cost increase
Solution Approach 1:
The invention creates a universal polymer matrix system that can accommodate multiple types of domains with different active substances and release characteristics. This multi-functional platform allows precise release profile control without requiring completely different polymer systems for each application, reducing overall complexity
Solution Approach 2:
The invention uses composite materials by combining a polymer matrix with embedded domains containing active substances. This composite structure enables precise release control through the interaction between matrix and domain properties, achieving zero-order release without requiring complex single-material systems
3Manufacturing precision
If zero-order release systems are created using conventional methods, then release precision is improved, but manufacturing difficulty and cost increase significantly
Solution Approach 1:
The invention performs preliminary action by pre-forming domains with controlled active substance concentration and distribution within the polymer matrix during manufacturing. This preliminary structuring enables zero-order release to occur automatically during use without requiring complex in-situ control mechanisms, simplifying manufacturing
Solution Approach 2:
The invention achieves zero-order release by changing key parameters of the polymer matrix and domain structure, such as domain size, concentration, and interfacial properties. These parameter modifications enable precise release control through straightforward formulation adjustments rather than complex manufacturing processes
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 approach enables controlled and sustained release of active substances, preventing the initial burst effect and allowing for precise delivery over time, with the ability to adjust release kinetics between zero-order and first-order profiles, enhancing the efficacy and cost-effectiveness of drug delivery systems.
Implementation Method 1
the composites proved to absorb significant amounts of liquid water (up to 1850% of sample mass)
Implementation Method 2
active substances are released from the elastomer matrices, upon contact with aqueous media
Implementation Method 3
The discrete glycerol domains embedded within a silicone matrix act as reservoirs for releasable substances
Data Source
AI summary
Herein is disclosed an elastomeric silicone composition comprising at least a first and a second glycerol phase which are distinct from each other and a method of making the same. The elastomeric compositions are special therein that zero-order active substance release can reversibly be obtained by modifying the glycerol content of the silicone composition.