Polymer Particles With Hydrolytic Linkages for Controlled Drug Release
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Solution Overview
Problem
Existing technologies lack effective methods for controlled, sustained delivery of pharmaceutical agents to diseased sites within the body, particularly through intravascular routes, and do not adequately address the need for biostable or biodegradable polymer particles that can release agents in a controlled manner.
Innovation Solution
Development of polymer particles, including hydrogel particles, composed of monomers, crosslinkers, and polymerizable pharmaceutical agents, which are designed to be biostable or biodegradable, allowing for controlled release of pharmaceutical agents through hydrolytic, oxidative, or reductive linkages, and are suitable for intravascular delivery using microcatheters.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If polymer particles are designed for controlled release of pharmaceutical agents, then the duration of action is improved, but the device complexity increases due to the need for specific polymer compositions and degradation mechanisms
Solution Approach 1:
The patent applies parameter changes by modifying the polymer composition parameters (monomer types, crosslinker ratios, molecular weight) and degradation parameters (hydrolytic, oxidative, reductive linkage rates) to achieve controlled release profiles. By systematically varying these parameters, the invention achieves different release durations and rates without fundamentally changing the particle structure, thus managing complexity through parameter optimization rather than structural complexity.
Solution Approach 2:
The invention uses composite materials by combining multiple polymer components (monomers, crosslinkers, pharmaceutical agents) into a unified particle system. This composite structure allows the particle to exhibit multiple functions (structural integrity, controlled degradation, drug loading, and release) simultaneously, resolving the contradiction by integrating complexity into a cohesive material system rather than separate components.
2Productivity
If polymer particles use hydrolytically degradable linkages for agent release, then the controlled release capability is improved, but the stability of the particle during delivery is worsened
Solution Approach 1:
The patent applies local quality by creating spatial and functional differentiation within the particle. Different regions or aspects of the particle have different stability characteristics - the overall particle structure remains stable during delivery through biostable crosslinking, while specific hydrolytically degradable linkages are localized at the drug-polymer interface to enable controlled release. This local differentiation resolves the contradiction between stability and release rate.
Solution Approach 2:
The invention applies dynamics by designing the particle to transition from a stable state during delivery to a degradable state at the target site. The particle maintains structural integrity through biostable crosslinkers during circulation, then dynamically switches to controlled degradation through hydrolytic, oxidative, or reductive mechanisms when triggered by the tumor microenvironment, achieving both stability during transport and controlled release at destination.
3Object-affected harmful factors
If polymer particles are made biodegradable for safety, then the harmful factors generated by the object are reduced, but the mechanical strength and durability during delivery are worsened
Solution Approach 1:
The patent applies preliminary action by pre-configuring the particle with biodegradable components that remain dormant during delivery. The biodegradable polymer backbone and crosslinkers are prepared in advance to provide mechanical strength, then activated for degradation only after delivery to the target site through triggers like pH changes, enzymes, or redox conditions in the tumor microenvironment. This preliminary preparation resolves the contradiction by ensuring strength when needed and biodegradability when appropriate.
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 particles enable controlled release of pharmaceutical agents at targeted sites, providing effective treatment by maintaining agent integrity during delivery and ensuring sustained release profiles, suitable for treating conditions like hypervascularized tumors and arteriovenous malformations.
Implementation Method 1
the polymers used herein can include at least one monomer amenable to polymerization, at least one crosslinker, and at least one pharmaceutical agent chemically bonded to the particle with a hydrolytically degradable linkage
Implementation Method 2
the pharmaceutical agent can be a polymerizable pharmaceutical agent. As the hydrolytic linkage is broken, the pharmaceutical agent can be controllably released from the polymer particle
Data Source
AI summary
Described are polymers and methods of forming and using same.