Chelating Complex Micelles for Controlled Drug Release
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Solution Overview
Problem
Current methods for controlling drug release rates in vivo are limited by the inability to simultaneously regulate distribution and release timing effectively, often resulting in decreased drug concentration and toxicity in non-target organs, and require significant alterations in pH or temperature, which are clinically impractical.
Innovation Solution
The use of chelating complex micelles (CCM) comprising a drug molecule, polymer ligand, and metal core, with a specific metal chelator administered to trigger drug release by chelating the metal core, allowing for controlled release rates and concentrations through varying administration times and routes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If pH or temperature is altered to accelerate drug release rate, then drug release rate is improved, but body fluid stability deteriorates due to limited pH range (0.1-0.2) and temperature tolerance (2°C)
Solution Approach 1:
The patent changes the chemical parameter of the system by introducing a metal chelator that specifically binds to the metal core, triggering drug release through chemical complexation rather than physical parameter changes like pH or temperature. This allows controlled release without compromising body fluid stability.
2Duration of action of moving object
If drug dosage is prolonged to extend release duration, then duration of action is improved, but release rate control deteriorates leading to unexpected time points and compromised drug effects
Solution Approach 1:
The patent incorporates the metal chelator into the micelle structure beforehand, creating a pre-assembled chelating complex micelle where the chelator is positioned to bind the metal core. This preliminary arrangement enables controlled triggering of drug release at specific times without compromising duration control.
Solution Approach 2:
The metal chelator acts as an intermediary that mediates between the metal core and the drug molecule. By binding to the metal core, the chelator triggers controlled drug release, allowing precise regulation of both release rate and duration without unexpected time points.
3Productivity
If drug concentration is increased in target organ to improve efficacy, then therapeutic effect is improved, but toxicity in non-target organs deteriorates due to excess distribution
Solution Approach 1:
The patent creates local quality differentiation by designing a micelle system where drugs are bound to the metal core only at the target site after chelator triggering. This ensures high drug concentration locally in the target organ while minimizing distribution to non-target organs, thereby improving therapeutic effect without increasing toxicity.
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
This method enables precise control over drug release rates and concentrations, reducing toxicity and improving efficacy by allowing targeted drug delivery and adjusting release timing and duration, while maintaining drug potency and prolonging half-life.
Implementation Method 1
a specific metal chelator administered to trigger drug release by chelating the metal core
Data Source
AI summary
This invention provides the controlled-release method for a pharmaceutical composition comprising of metals in the drug carrier. The specific chelator is used to trigger the release of active pharmaceutical ingredients from chelating complex micelles. The drug release rate and half-life can also be controlled by manipulating the dosing sequence and the concentration of metal and specific chelator.