Amphiphilic Block Copolymer Micelle Stabilization via Ionizable Salt
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Solution Overview
Problem
Existing methods for stabilizing poorly water-soluble drug-containing amphiphilic block copolymer micelles face challenges such as poor biodegradability, biocompatibility, and stability issues, particularly during in vivo applications, and the solvent evaporation process is limited by the selection of solvents and can cause degradation of pharmaceutically active ingredients.
Innovation Solution
A method involving dissolving poorly water-soluble drugs and amphiphilic block copolymers in an organic solvent and adding an aqueous solution containing an ionizable salt to form polymeric micelles, which improves the stability and biodegradability of the micelle composition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If crosslinking is used to stabilize polymeric micelles, then micelle stability is improved, but biodegradability deteriorates
Solution Approach 1:
The patent changes the chemical parameters of the copolymer by incorporating hydrolyzable bonds (ester, amide, carbamate groups) into the polymer backbone, enabling controlled degradation while maintaining micelle stability through careful selection of hydrophilic and hydrophobic block ratios and crosslinking density
Solution Approach 2:
The patent creates composite micelle structures combining hydrophilic blocks (polyethylene oxide, polypropylene oxide) with hydrophobic blocks (polylactic acid, polyglycolic acid, polyamino acid) that have different degradation rates, achieving both stability and biodegradability through material composition
2Quantity of substance
If solvent evaporation process is used to encapsulate drugs, then drug loading capacity is improved, but drug degradation occurs
Solution Approach 1:
The patent changes the temperature parameter by conducting micelle formation at low temperatures (4-25°C) rather than high temperature evaporation, preventing drug degradation while achieving effective drug encapsulation through controlled self-assembly
Solution Approach 2:
The patent uses an intermediary approach by first dissolving drugs and polymers in organic solvent, then adding aqueous solution to induce micelle formation, avoiding direct high-temperature evaporation that degrades drugs
3Stability of the object's composition
If crosslinkers are applied to stabilize micelles, then micelle structure stability is improved, but biocompatibility deteriorates
Solution Approach 1:
The patent changes the chemical nature of crosslinking by using hydrolyzable crosslinking mechanisms inherent in the polymer structure (ester, amide bonds) rather than introducing external crosslinkers, achieving stability while maintaining biocompatibility through biologically benign bond types
Solution Approach 2:
The patent employs temporary crosslinking through hydrolyzable bonds that provide structural stability during circulation but degrade in the body, effectively using transient stabilization that disappears after serving its purpose
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 approach results in a stabilized poorly water-soluble drug-containing amphiphilic block copolymer micelle composition with enhanced stability, preventing rapid drug release and maintaining stability for extended periods, even when reconstituted into an injection formulation.
Implementation Method 1
adding an aqueous solution containing an ionizable salt thereto to form polymeric micelles
Implementation Method 2
adding an aqueous solution containing an ionizable salt thereto to form polymeric micelles
Data Source
AI summary
A method for stabilizing a poorly water-soluble drug-containing amphiphilic block copolymer micelle composition via simplified steps in short time is described. Also described is a stabilized poorly water-soluble drug-containing amphiphilic block copolymer micelle composition having improved stability.