Sustained-Release PLGA Microspheres for Therapeutic Gas Delivery
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Solution Overview
Problem
Current therapeutic agents like diallyl trisulfide and magnesium have short half-lives, limiting their ability to provide sustained, long-term therapeutic effects in treating ischemia and oxidative stress-related conditions due to rapid reaction rates and short durations of action.
Innovation Solution
A sustained-release composition using diallyl trisulfide or magnesium as precursors carried by a poly lactic-co-glycolic acid (PLGA) copolymer carrier, which slows down the release of hydrogen sulfide or hydrogen, allowing for continuous production and prolonged therapeutic effect through single emulsification and microsphere formation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If diallyl trisulfide or magnesium is used as a therapeutic agent, then the therapeutic gas (hydrogen sulfide or hydrogen) can be produced to scavenge ROS, but the half-life is too short to provide long-term therapeutic effect
Solution Approach 1:
The therapeutic precursor (diallyl trisulfide or magnesium) is encapsulated within PLGA microspheres, creating a nested structure where the active agent is contained inside a sustained-release matrix. This nesting allows the precursor to be protected and released gradually over time, extending the therapeutic effect from minutes to days or weeks.
Solution Approach 2:
The invention changes the physical and chemical parameters of the therapeutic system by incorporating the precursor into a polymeric matrix with controlled degradation properties. The PLGA matrix degradation rate controls the release kinetics, transforming the rapid-release scenario into a sustained-release system with tunable duration parameters.
2Productivity
If magnesium reacts with water to produce hydrogen, then hydrogen can be generated for therapeutic effect, but the reaction rate is too fast to provide sufficient hydrogen at lesion zone for prolonged duration
Solution Approach 1:
The PLGA matrix acts as an intermediary between the magnesium precursor and water, controlling their interaction. The matrix allows gradual water penetration and controlled magnesium exposure, mediating the reaction rate to provide sustained hydrogen generation rather than rapid uncontrolled reaction.
Solution Approach 2:
The PLGA microsphere forms a flexible polymeric shell around the magnesium precursor, controlling the interface between the reactive metal and aqueous environment. This shell provides controlled permeability to water and products, enabling sustained 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 sustained-release composition effectively maintains therapeutic gas levels for extended periods, promoting angiogenesis and reducing oxidative stress in ischemic tissues, achieving a long-term therapeutic effect.
Implementation Method 1
a sustained-release composition includes a precursor and a carrier. The precursor is diallyl trisulfide or magnesium, and the carrier includes a poly lactic-co-glycolic acid (PLGA) copolymer for carrying the precursor with an efficient amount
Implementation Method 2
hydrogen sulfide (H2S) is recognized as a gaseous signaling molecule and can be endogenously produced in a variety of tissues and cells of mammals
Implementation Method 3
magnesium (Mg) can be employed as a hydrogen precursor and react with water to produce magnesium hydroxide precipitate and hydrogen molecules. The reaction as mentioned above is performed according to the formula (1): Mg+2H2O→Mg(OH)2+H2 (g)
Implementation Method 4
The step of performing the single emulsification is achieved by mixing the first solution and the second solution to form the sustained-release composition
Data Source
AI summary
A sustained-release composition is provided in the present disclosure for producing a therapeutic gas, such as hydrogen sulfide or hydrogen. The sustained-release composition includes a precursor and a carrier. The precursor is diallyl trisulfide or magnesium, and the carrier includes a poly lactic-co-glycolic acid copolymer for carrying the precursor with an efficient amount.