Controlled Release Composition Using Matrix and Microparticles
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Solution Overview
Problem
Microparticle-based controlled release compositions face issues such as aggregation, high solvent requirements, and difficulty in measuring drug release rates within tissues, making them impractical for sustained medication delivery, especially in solid tumors.
Innovation Solution
A controlled release composition comprising a matrix linked with microparticles, where the microparticles have a higher initial melting temperature than the matrix, allowing for controlled drug release and reducing solvent usage, with the microparticles being uniformly or randomly distributed within the matrix to enhance stability and release profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but microparticles form aggregates affecting composition properties
Solution Approach 1:
The patent introduces a matrix material as an intermediary substance that embeds and stabilizes microparticles, preventing their aggregation. The matrix acts as a spacer and protective medium, maintaining uniform distribution of microparticles while enabling sustained drug release over time.
2Duration of action of stationary object
If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but large amount of solvent is required (80-90% solvent ratio)
Solution Approach 1:
The patent changes the physical state and composition parameters by using a matrix material with specific melting temperature characteristics. The matrix material is selected to have a melting temperature higher than the microparticle material, allowing the system to be processed in a molten state and then solidified, thereby eliminating the need for large amounts of solvent while maintaining sustained release properties.
3Duration of action of stationary object
If microparticle-based controlled release composition is implanted, then sustained release of medicament is achieved, but microparticles move easily within tissue making drug release rate measurement impractical
Solution Approach 1:
The patent uses the matrix material as a counterbalancing structure that anchors and immobilizes the microparticles within the tissue implantation site. The matrix provides mechanical stability and prevents microparticle migration, creating a stable environment where drug release rate can be accurately measured and controlled.
4Duration of action of stationary object
If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but it is impractical for injection into solid tumors
Solution Approach 1:
The patent transforms the physical state of the composition by utilizing a matrix material that can be melted above its melting temperature. This allows the composition to be injected in a molten, fluid state into solid tumors, and then solidifies in situ to provide sustained release, thereby combining the ease of injection with the benefit of sustained release without requiring large amounts of solvent.
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 composition provides a stable and controlled release of active agents, reducing the frequency of dosing and improving patient compliance, while minimizing solvent use and facilitating precise drug delivery within tissues.
Implementation Method 1
the first material comprises an initial melting temperature TH; the second material comprises a complete melting temperature TL; ΔT=TH−TL; and ΔT>0
Data Source
AI summary
The present disclosure provides a controlled release composition comprising a plurality of microparticles and a matrix, wherein: the plurality of microparticles comprises a first material; the matrix comprises a second material; and the melting temperature of the first material is higher than the melting temperature of the second material. Also provided are methods of making and using the same.


