Naltrexone Microparticles Sustained Release via PLGA
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Solution Overview
Problem
Current naltrexone delivery systems face challenges in achieving sustained release for longer than one month, requiring frequent injections and having high attrition rates due to compliance issues, and they often require surgical procedures for implant-based systems, which come with risks and complications.
Innovation Solution
Development of injectable, controlled-release naltrexone microparticles using biodegradable polymers like PLGA, prepared through solvent extraction/evaporation of an oil-in-water emulsion, allowing for subcutaneous or intramuscular administration with unique release profiles lasting up to 100 days, enabling smaller needle diameters and stable therapeutic levels.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If implant-based delivery systems are used to achieve longer release profiles, then duration of action is improved, but device complexity and surgical requirements worsen
Solution Approach 1:
The patent extracts the drug delivery function from complex implant-based systems and transfers it to simple injectable microparticles. The microparticles are formulated to be administered via standard injection techniques without surgical intervention, while maintaining extended release profiles through controlled polymer degradation and drug diffusion mechanisms
Solution Approach 2:
The patent changes the physical and chemical parameters of the microparticles, including particle size distribution (d50,volume of 108.49 μm, d50,population of 58.46 μm), polymer composition (PLGA ratios), and drug loading concentrations, to optimize both the extended release duration and the ability to be administered through standard needle gauges without surgical procedures
2Ease of operation
If larger needle diameters are used for microparticle injection, then ease of operation is improved, but device complexity worsens
Solution Approach 1:
The patent applies local quality by creating a specific microparticle size distribution profile where particles are engineered with precise dimensional characteristics (d50,volume of 108.49 μm, d50,population of 58.46 μm) that enable them to flow through standard 20 gauge needles while maintaining their structural integrity and controlled release properties
Solution Approach 2:
The patent introduces dynamic characteristics by formulating microparticles with specific size distributions that allow them to adapt to the injection process, flowing through needles of standard gauge while maintaining their functional properties for extended release over 4 weeks or longer
3Stability of the object's composition
If frequent injections are administered to maintain therapeutic levels, then stability of drug concentration is improved, but loss of time and patient compliance worsen
Solution Approach 1:
The patent implements continuous useful action by formulating microparticles that provide sustained release of naltrexone over extended periods (4 weeks or longer), maintaining stable therapeutic drug levels through controlled polymer degradation and drug diffusion, thereby eliminating the need for frequent injections and improving patient compliance
Solution Approach 2:
The patent applies preliminary action by pre-encapsulating the drug in biodegradable polymer matrices with controlled degradation rates, so that the therapeutic agent is released continuously over an extended period following a single injection, rather than requiring repeated administrations to maintain stable drug levels
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 microparticle formulation provides sustained release of naltrexone for 8 to 12 weeks, reducing the need for frequent injections, improving patient compliance, and offering stable therapeutic levels with minimal initial burst release, while being biocompatible and suitable for administration through thinner needles.
Implementation Method 1
releasing naltrexone for a period of about four weeks
Implementation Method 2
naltrexone encapsulated in biodegradable microparticles
Implementation Method 3
prepared through solvent extraction/evaporation of an oil-in-water emulsion
Implementation Method 4
prepared through solvent extraction/evaporation of an oil-in-water emulsion
Data Source
AI summary
The present disclosure relates to naltrexone sustained release microparticle delivery systems for the treatment of diseases ameliorated by naltrexone. The injectable microparticle delivery system includes naltrexone encapsulated in biodegradable microparticles administered in a pharmaceutically acceptable vehicle.