Poly(ester urea) Synthesis for Drug Delivery Complexation

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Solution Overview

Problem

Current poly(ester urea)s for drug delivery lack optimal water solubility and complexation efficiency, necessitating the development of novel amino acid and diol combinations to enhance their biocompatibility and effectiveness in forming nanoscale drug delivery particles.

Innovation Solution

The development of poly(ester urea)s with specific structures incorporating various amino acid monomers and diols, such as lysine, arginine, and diethylene glycol, to improve water solubility and complexation efficiency, allowing for the formation of polyplexes in the form of micelles, liquid polyplexes, or thin-film coatings for enhanced drug delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional poly(ester urea)s are used for drug delivery, then basic biocompatibility is achieved, but water solubility and complexation efficiency are insufficient

Engineering Contradiction:
Improvecomplexation efficiencyVSAvoidwater solubility
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical parameters of poly(ester urea)s by incorporating specific amino acid monomers (lysine, arginine, aspartic acid) and diol linkers (diethylene glycol, triethylene glycol) to optimize water solubility and complexation efficiency. This involves changing the compositional parameters of the polymer to achieve desired solubility and binding properties for drug delivery applications

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite poly(ester urea) structures by combining multiple amino acid monomers and diol linkers in specific ratios. These composite materials integrate hydrophilic components (for solubility) with functional groups (for complexation), achieving both improved water solubility and enhanced drug complexation efficiency simultaneously

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If novel amino acid and diol combinations are developed to improve water solubility, then complexation efficiency increases, but material complexity and synthesis difficulty increase

Engineering Contradiction:
Improvewater solubilityVSAvoidpolymer structure complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent divides the poly(ester urea) structure into distinct functional segments: amino acid monomer units (providing solubility and complexation functionality) and diol linker units (providing structural flexibility and solubility). This segmentation allows independent optimization of each component's properties while maintaining overall polymer functionality

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs universal building blocks (standard amino acids and common diols) that can be combined in various ratios to create multiple poly(ester urea) variants with different solubility and complexation profiles. This multi-functional approach allows a single set of monomers to serve multiple drug delivery applications by adjusting composition rather than designing entirely new polymers

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 optimized poly(ester urea)s enable improved complexation and delivery of therapeutic, diagnostic, and prophylactic agents, offering enhanced biocompatibility and tunable properties for fine-tuning drug delivery applications.

Implementation Method 1

Polyelectrolyte complexation has been demonstrated as an effective method for the formation of nanoscale drug delivery particles including micelles, polyplexes, and thin-film coatings.

Methodology Applied
Scientific EffectPolyelectrolyte complexation: Electrostatic Induction

Data Source

PatentUS20230312827A1Synthesis of novel poly(ester urea)s for drug delivery
Publication Date: 2023.10.05 MASSACHUSETTS INST OF TECH
  • US20230312827A1 patent drawing
  • US20230312827A1 patent drawing
  • US20230312827A1 patent drawing

AI summary

Disclosed are poly(ester urea)s containing two or more units containing two amino acid monomers linked by a linker. At least two units of the poly(ester urea)s are covalently bonded via a urea bond. Suitable amino acid monomers are lysine, arginine, aspartic acid, phenylalanine, or a side chain protected derivative thereof, and suitable linkers are selected from a 1,4-butane diol group, a 1,6-hexane diol group, diethylene glycol group, a triethylene glycol group, or an N-methyl diethanolamine group. The poly(ester urea)s are used to form polyplexes for the improved complexation and delivery of drugs to a subject in need thereof.