PLGA Microsphere Injectable for Long-Acting Dual Parasite Control
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Solution Overview
Problem
Current parasitic treatments for animals lack effective, long-lasting, and easily administered injectable compositions that provide sustained efficacious concentrations of isoxazoline and macrocyclic lactones in the blood plasma.
Innovation Solution
A novel extended-release injectable polymeric microsphere composition containing both isoxazoline and macrocyclic lactone, formulated with PLGA or PLA polymers, offering a stable and versatile drug release mechanism.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a single injectable composition contains both isoxazoline and macrocyclic lactone, then the duration of action and versatility of treatment is improved, but the device complexity and formulation difficulty increase
Solution Approach 1:
The patent combines two different antiparasitic compounds (isoxazoline and macrocyclic lactone) into a single injectable microsphere formulation, allowing both drugs to be administered simultaneously through one injection site. This merging approach extends the duration of action by providing sustained release of multiple active ingredients while treating different parasite types with a single treatment event.
Solution Approach 2:
The formulation uses composite microsphere structures containing both isoxazoline and macrocyclic lactone compounds embedded in a biodegradable polymer matrix. This composite material approach enables controlled release kinetics for both drugs simultaneously, resolving the complexity of creating a multi-drug formulation while maintaining simplicity of administration.
2Quantity of substance
If the microsphere mass/number is increased to achieve higher dose, then the dosing flexibility is improved, but the injection volume and administration complexity increase
Solution Approach 1:
The patent achieves dose flexibility by changing the concentration parameters of active ingredients within the microspheres rather than changing the physical number or size of microsphere particles. By adjusting the drug loading percentages and release kinetics parameters, the formulation provides flexible dosing (e.g., 6-month vs 12-month efficacy) while maintaining a consistent, simple injection volume and administration procedure.
3Duration of action of moving object
If the injectable composition provides extended-release, then the duration of action is improved, but the manufacturing precision and stability requirements increase
Solution Approach 1:
The patent uses biodegradable polymer matrices as intermediary materials that control the release kinetics of both isoxazoline and macrocyclic lactone compounds. These polymer intermediaries provide a stable, controllable mechanism for extended-release delivery, reducing the manufacturing precision requirements by using well-established polymer degradation kinetics rather than requiring precise control of drug particle size or composition variations.
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
Provides prolonged efficacy against ectoparasites and endoparasites, preventing tick-borne diseases with a single subcutaneous injection every 6-12 months, maintaining effective drug levels in the animal's bloodstream.
Implementation Method 1
The polymeric composition is prepared as a suspension composition for subcutaneous injection... polymeric microspheres containing both an isoxazoline and a macrocyclic lactone... poly (D,L-lactide-co-glycolide) (PLGA) polymer or a poly (D,L-lactic acid) (PLA) polymer
Data Source
AI summary
The invention describes an extended-release composition comprising PLGA or PLA polymeric microspheres comprising an isoxazoline, preferably sarolaner, and a macrocyclic lactone, preferably moxidectin, and wherein the composition further comprises at least one pharmaceutically acceptable excipient; and uses thereof.