Echinochrome A Polymeric Micro-/Nanofibers for Stable Controlled Release
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Solution Overview
Problem
Echinochrome A's poor solubility and stability in aqueous solutions limit its use in pharmaceutical formulations, prohibiting oral, buccal, nasal, or transdermal administration, and existing formulations lack controlled release and targeted delivery capabilities.
Innovation Solution
Development of polymeric micro-/nanofibers incorporating echinochrome A using biocompatible polymers like polyvinylpyrrolidone and polycaprolactone, fabricated via electrospinning, offering controlled release and targeted delivery based on pH sensitivity and hydrophilicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If echinochrome A is formulated as an isotonic solution of its di- and tri-sodium salts for injection, then it can be administered parenterally, but its poor solubility and sensitivity to oxidation severely restrict its use and prohibit oral, buccal, nasal or transdermal administration
Solution Approach 1:
The patent uses cyclodextrins as intermediary molecules that form inclusion complexes with echinochrome A. The cyclodextrin cavity encapsulates the echinochrome A molecule, protecting it from oxidation while the external hydroxyl groups enhance water solubility. This mediator approach enables multiple routes of administration while maintaining stability.
Solution Approach 2:
The invention creates a composite pharmaceutical formulation consisting of cyclodextrin inclusion complexes with echinochrome A. This composite material combines the protective and solubilizing properties of cyclodextrins with the therapeutic activity of echinochrome A, resolving the contradiction between stability and ease of administration.
2Reliability
If echinochrome A is incorporated in carrageenan matrices to increase stability and solubility, then stability and solubility are improved, but the release is uncontrolled and duration of action is limited
Solution Approach 1:
The patent modifies the chemical structure of cyclodextrins by introducing various substituents (hydrophilic, hydrophobic, charged groups) to change the properties of the inclusion complex. This allows tuning of release kinetics and extending duration of action while maintaining stability. Different cyclodextrin derivatives provide controlled release profiles.
Solution Approach 2:
The invention creates heterogeneity in the cyclodextrin structure by introducing different functional groups at specific positions. This local modification of cyclodextrin properties allows control over release rate and duration while maintaining the core stabilizing function of the cyclodextrin cavity.
3Duration of action of moving object
If echinochrome A is used in single-polymer micro-/nanofibers, then prolonged release is achieved at specific pH, but the formulation lacks versatility for targeted delivery to different locations
Solution Approach 1:
The patent develops cyclodextrin-based formulations that can function across multiple routes of administration (oral, buccal, nasal, transdermal, parenteral) and target different locations. The cyclodextrin inclusion complex serves as a universal delivery platform that maintains stability and enables prolonged release regardless of the administration route, providing versatility for targeted delivery to cardiovascular, ophthalmic, gastrointestinal, and other tissues.
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 micro-/nanofibers provide enhanced stability and solubility of echinochrome A, enabling prolonged release and targeted delivery for various therapeutic applications, including cardiovascular, ophthalmic, inflammatory, and cancer treatments.
Implementation Method 1
fabricated via electrospinning
Data Source
AI summary
The invention relates to the development of a new pharmaceutical formulation for use as a medicament, in particular in anti-inflammatory diseases, and comprises of polymeric micro-/nanofibers incorporating echinochrome A. The composition provides increased stability and solubility, as well as controlled release for echinochrome A, while offering the potential for its targeted delivery.