Deslorelin Microparticles for Sustained Chemical Castration
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Solution Overview
Problem
Existing methods of chemical castration using deslorelin cause pain in animals due to direct injection, and there is a need for a sustained-release formulation that maintains the castration effect for an extended period without causing discomfort.
Innovation Solution
Sustained-release microparticles containing deslorelin and a biodegradable polymer are prepared through a microfluidic emulsification method, forming O 1 (Oil)/O 2 (Oil)/W(Water) or W 1 (Water)/O(Oil)/W 2 (Water) emulsions with a controlled diameter of 25 to 140 µm, ensuring even distribution of deslorelin within the microparticles.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If deslorelin is injected directly into the animal body as an implant, then the chemical castration effect is achieved, but severe pain is caused to the animal during administration
Solution Approach 1:
The patent segments the deslorelin delivery system into microparticles (25-140 μm diameter) embedded within a biodegradable polymer matrix. This segmentation allows the drug to be delivered in distributed micro-doses rather than a single large implant, reducing administration pain while maintaining the chemical castration effect.
Solution Approach 2:
The patent changes the physical parameters of deslorelin delivery by forming it into microparticle suspension that can be administered via subcutaneous injection rather than as a large implant. This parameter change from implant to microparticle suspension fundamentally alters the administration method from painful surgical implantation to minimally painful injection.
2Reliability
If deslorelin is administered to achieve chemical castration, then the castration effect is obtained, but the effect duration is insufficient and requires repeated administration
Solution Approach 1:
The patent achieves continuous useful action by embedding deslorelin microparticles within a biodegradable polymer matrix that controls drug release over time. The polymer degradation rate is synchronized with drug release, providing sustained castration effect for 2-8 months without requiring repeated administrations.
Solution Approach 2:
The patent uses composite materials by combining deslorelin microparticles with biodegradable polymer matrix. This composite structure allows the polymer to control the release kinetics of deslorelin, extending the duration of action from days to months while maintaining reliable castration effect.
3Ease of operation
If microparticles with small diameter are used for subcutaneous injection, then administration comfort is improved, but the sustained-release effect may be reduced
Solution Approach 1:
The patent optimizes the microparticle diameter parameter to the specific range of 25-140 μm. This parameter change balances two competing requirements: small enough diameter for comfortable subcutaneous injection and large enough size to contain sufficient deslorelin load and provide sustained release over 2-8 months.
Solution Approach 2:
The composite structure of deslorelin microparticles within the polymer matrix allows small microparticle diameter for comfort while the aggregated matrix structure provides the volume needed for sustained release. The polymer matrix acts as a reservoir that maintains drug release duration despite small individual particle size.
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 microparticles provide a pain-free chemical castration effect lasting 2 to 36 months and effectively remove boar taint in male pigs by continuous deslorelin release for 2 to 8 months, alleviating animal suffering and facilitating ethical handling.
Implementation Method 1
a method for preparing sustained-release microparticles containing deslorelin... injecting the first mixture of the step 1) into a channel in a linear direction... injecting the second mixture of the step 2) into a channel formed on either side or one side so as to form a cross-point... to prepare microparticles in which deslorelin is evenly distributed
Data Source
Figure 1~2
AI summary
According to sustained-release microparticles containing deslorelin, and a preparation method therefor, of the present invention, sustained-release microparticles containing deslorelin in a formulation for subcutaneous administration are provided so that pain can be relieved during administration to animals, and a chemical castration effect can last for 2 to 36 months. In addition, the present invention is effective as a chemical castration agent for 2 to 8 months so as to have an excellent of removing boar taint.