Apixaban Polymer Microspheres for Stable High-Load Encapsulation
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Solution Overview
Problem
Existing methods fail to effectively encapsulate Apixaban in biocompatible polymer microspheres due to low solubility and high crystallization tendencies, leading to low bioavailability and gastrointestinal bleeding risks with oral administration.
Innovation Solution
A method involving the addition of fatty acids or triglycerides to a dispersed phase containing Apixaban and biocompatible polymers like PLGA, PLA, and PCL, using a microfluidic process to stabilize high drug content encapsulation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If Apixaban is orally administered, then it can be conveniently taken, but bioavailability is low due to low water solubility
Solution Approach 1:
The patent segments the drug delivery system by encapsulating Apixaban within biocompatible polymer microspheres, separating the drug from direct contact with gastrointestinal fluids that limit its solubility. This microencapsulation approach allows the drug to be delivered in a controlled manner while improving bioavailability through alternative administration routes.
Solution Approach 2:
The patent introduces biocompatible polymers as intermediary materials that solubilize and protect Apixaban during delivery. These polymers act as mediators between the poorly water-soluble drug and the biological system, enabling enhanced absorption and reduced gastrointestinal irritation.
2Ease of operation
If Apixaban is orally administered, then it can be taken easily, but gastrointestinal bleeding occurs due to local anticoagulant effects and corrosive actions
Solution Approach 1:
The patent extracts Apixaban from direct contact with the gastrointestinal tract by encapsulating it within polymer microspheres. This removal of the drug from the harsh gastrointestinal environment eliminates local corrosive actions and non-coagulation-related biological actions that cause gastrointestinal bleeding, while still allowing systemic anticoagulant effects to occur.
Solution Approach 2:
The patent employs biocompatible polymers that are designed to degrade completely after delivering the drug. These temporary carriers provide protection during transit and administration, then naturally decompose in the body, eliminating long-term harmful effects while maintaining ease of administration.
3Ease of manufacture
If conventional microsphere preparation methods are used, then the process is simple, but Apixaban crystallizes and cannot be stably encapsulated in high content
Solution Approach 1:
The patent optimizes critical parameters including polymer selection (PLGA, PLA, or PCL with specific molecular weights), solvent systems (dichloromethane, chloroform, or ethyl acetate), and processing conditions (emulsion formation, solvent evaporation temperature and time) to prevent Apixaban crystallization while maintaining high encapsulation efficiency and stability.
Solution Approach 2:
The patent uses composite material systems combining Apixaban with biocompatible polymers in specific ratios, creating a synergistic formulation where the polymer matrix prevents drug crystallization while enabling stable encapsulation. The composite approach integrates multiple functional components to achieve both manufacturability and product quality.
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
Stable encapsulation of high Apixaban content in microspheres for sustained release, enabling intramuscular or subcutaneous administration, improving bioavailability and reducing gastrointestinal bleeding risks.
Implementation Method 1
preparing microspheres using a microfluidic method, wherein the biocompatible polymer is any one or more selected from the group consisting of polylactic-co-glycolic acid (PLGA), polylactic acid (PLA), and polycaprolactone (PCL)
Implementation Method 2
The known preparation methods for microspheres include i) a solvent evaporation method
Data Source
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AI summary
The present invention relates to a method for preparing biocompatible polymer-based Apixaban-loaded microspheres. More specifically, the present invention relates to a method for preparing biocompatible polymer-based Apixaban-loaded microspheres, comprising: i) adding a fatty acid or triglyceride to a dispersed phase; and ii) preparing microspheres using a microfluidic method. The method for preparing biocompatible polymer-based Apixaban-loaded microspheres of the present invention can be effectively used in the preparation of microspheres in which Apixaban is stably encapsulated in high contents.