Biocompatible Polymer Apixaban Microspheres via Microfluidics
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Solution Overview
Problem
Apixaban, a drug used to prevent blood clots and coagulation, has low bioavailability due to low water solubility and can cause gastrointestinal bleeding when orally administered, necessitating a novel administration route to improve bioavailability and reduce bleeding risks.
Innovation Solution
Preparation of biocompatible polymer-based Apixaban-loaded microspheres by adding a fatty acid or triglyceride to a dispersed phase and using a microfluidic method for encapsulation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Apixaban is orally administered, then it can prevent blood clots and coagulation, but the absorption is inhibited due to low water solubility resulting in only about 50% bioavailability
Solution Approach 1:
The patent changes the physical form of Apixaban from a simple oral tablet to a microsphere formulation with controlled size (1-100 μm diameter) and specific surface area-to-volume ratio. This parameter change enables the drug to be administered via injection rather than oral route, fundamentally altering absorption characteristics and achieving nearly 100% bioavailability by bypassing gastrointestinal absorption limitations
Solution Approach 2:
The patent creates a composite material system where Apixaban is encapsulated within biocompatible polymer microspheres. The microsphere structure comprises a polymer matrix (such as PLGA, PLA, or PCL) that encapsulates Apixaban molecules, providing controlled release while improving overall drug delivery efficiency and bioavailability compared to raw Apixaban administration
2Reliability
If Apixaban is orally administered, then it exerts anticoagulant effects, but gastrointestinal bleeding may be caused by local anticoagulant effects and direct corrosive actions
Solution Approach 1:
The patent extracts Apixaban from the gastrointestinal administration environment and delivers it directly into the systemic circulation via intramuscular or subcutaneous injection. This removes the drug from contact with the gastrointestinal tract entirely, eliminating local corrosive actions and local anticoagulant effects that cause gastrointestinal bleeding while preserving the desired systemic anticoagulant effect
Solution Approach 2:
The biocompatible polymer microsphere acts as an intermediary carrier that encapsulates Apixaban and controls its release into the bloodstream. This intermediary system allows the drug to bypass direct contact with gastrointestinal tissues, preventing harmful local effects while maintaining therapeutic anticoagulant activity through controlled systemic delivery
3Ease of manufacture
If conventional microsphere preparation methods are used, then microspheres can be formed, but Apixaban has never been successfully developed as a microsphere formulation using these methods
Solution Approach 1:
The patent applies preliminary action by pre-mixing Apixaban with the polymer solution in a specific ratio before microsphere formation, and by pre-optimizing the solvent system and emulsification conditions. This preliminary preparation ensures that Apixaban is properly distributed within the polymer matrix before the microsphere structure is formed, preventing aggregation and ensuring successful encapsulation
Solution Approach 2:
The patent systematically optimizes critical parameters including polymer molecular weight, drug-to-polymer ratio, solvent type and volume, emulsification speed, and crosslinking conditions. These parameter changes transform the conventional microsphere preparation process into a optimized protocol specifically suited for Apixaban, enabling successful encapsulation where previous methods failed
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 and improving bioavailability while reducing gastrointestinal bleeding.
Implementation Method 1
preparing microspheres using a microfluidic method
Implementation Method 2
adding a fatty acid or triglyceride to a dispersed phase
Data Source
AI summary
The present disclosure relates to a method for preparing biocompatible polymer-based Apixaban-loaded microspheres. More specifically, the present disclosure relates to a method for preparing biocompatible polymer-based Apixaban-loaded microspheres, where the method includes: 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 disclosure may be effectively used in the preparation of microspheres in which Apixaban is stably encapsulated in high contents.