Boronated Polymers for Acidic pH Drug Delivery
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Solution Overview
Problem
Existing drug delivery systems based on polymers with boronic acid groups are limited to basic pH conditions and cannot effectively deliver drugs at acidic pH levels, which are relevant in cellular transport processes such as in phagosomes and endosomes.
Innovation Solution
Development of boronated polymers with specific molecular structures that can form hydrogels and nanoparticles, capable of binding with glycoproteins and exhibiting enhanced transfection efficiency, allowing for reversible drug delivery triggered by pH, temperature, or carbohydrates, and showing improved endosomal escape properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If polymers with boronic acid groups are used for drug delivery, then the system can form hydrogels and interact with polyol systems, but the system is limited to basic pH conditions and cannot effectively deliver drugs at acidic pH levels
Solution Approach 1:
The patent modifies the chemical structure of boronic acid-containing polymers by introducing specific molecular structures (Formula I) that enable the polymer to maintain stability and functionality across a broader pH range, particularly at acidic pH levels where conventional boronic acid polymers fail. This structural parameter change allows the polymer to overcome the pH limitation while retaining its hydrogel-forming and drug delivery capabilities.
2Reliability
If conventional poly(amino ester)s are used for pH-triggered drug delivery, then the micro-particles can dissolve in acidic environments, but the system shows increased toxicity and limited transfection efficiency
Solution Approach 1:
The patent creates a composite polymer structure combining boronic acid groups with specific molecular architectures (Formula I) that integrate the pH-responsive behavior of poly(amino ester)s with the enhanced stability and reduced toxicity of boronic acid-containing polymers. This composite structure achieves effective pH-triggered drug delivery while minimizing the harmful effects of toxicity and improving transfection efficiency.
3Duration of action of stationary object
If boronic acid-containing polymers are cross-linked to form hydrogels, then the system can provide controlled drug release, but the system cannot achieve reversible drug delivery at acidic pH conditions
Solution Approach 1:
The patent introduces dynamic covalent chemistry through boronic acid ester bonds that can reversibly form and break down in response to pH changes. The specific molecular structure (Formula I) enables these bonds to remain stable at physiological pH for controlled drug release, while becoming reversible at acidic pH conditions, allowing the hydrogel to dynamically adapt its drug release behavior based on the environmental pH.
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 boronated polymers demonstrate lower toxicity, higher transfection efficiency, and the ability to form stable nanoparticles with enhanced endosomolytic properties, enabling effective drug delivery at acidic pH levels and providing controlled release mechanisms.
Implementation Method 1
boronic acid and boronic acids as well as polymers comprising boronic acid groups interact with polyol systems, e.g. polyvinyl alcohol, to form hydrogels
Implementation Method 2
In their cationic form, the poly(amino ester)s form complexes with DNA molecules or fragments thereof
Implementation Method 3
Upon exposure to an acidic environment, e.g. the endosome or the phagosome of a cell, the micro-particles dissolve or disrupt due to an enhanced solubility of the poly(amino ester) which is caused by hydrolysis of ester bonds in the polymer backbone
Data Source
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AI summary
The present invention relates to a boronated polymer according to Formula (1): a process for making the boronated polymer according to Formula (1), drug 10 delivery systems, aggregates, nanoparticles and hydrogels comprising the boronated polymer according to Formula (1).