PEG-AMP Conjugates Inhibit Biofilm Formation

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Solution Overview

Problem

Biofilms formed by pathogens such as Pseudomonas aeruginosa and Escherichia coli are difficult to eliminate due to their organized structure and resistance to hostile environments, including anti-microbial agents, posing challenges in various industries and medical applications.

Innovation Solution

Development of peptide conjugates comprising a polyethylene glycol (PEG) polymer linked to an antimicrobial peptide (AMP) with specific amino acid sequences, such as ILGPVLGLVSDTLDDVLGIL-COOH, which are used to coat surfaces or administered to prevent or treat infections by inhibiting biofilm formation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional anti-microbial agents are used, then bacterial growth can be inhibited, but biofilms become highly resistant and difficult to eliminate

Engineering Contradiction:

Improveanti-microbial effectivenessVSAvoidbiofilm resistance

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention combines polyethylene glycol (PEG) polymer with antimicrobial peptides (AMPs) to create a composite conjugate structure. The PEG-AMP conjugate integrates the biofilm-preventing properties of PEG with the potent antimicrobial activity of AMPs, achieving both biofilm inhibition and bacterial killing in a single composite material that overcomes the resistance developed against conventional agents alone

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The invention modifies the chemical and physical parameters of anti-microbial systems by conjugating AMPs to PEG polymers with specific molecular weights (1-50 kDa). This parameter change creates a new molecular entity with enhanced properties: the PEG portion prevents biofilm formation while the AMP portion provides potent bactericidal activity, achieving effectiveness against resistant biofilms

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If biofilms are allowed to form, then bacterial organization and stability increase, but elimination becomes extremely difficult

Engineering Contradiction:

Improvebiofilm stabilityVSAvoidbiofilm elimination

Core Design Contradiction:

Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The PEG-AMP conjugate applies preliminary anti-action by preventing biofilm formation in the first place. The PEG portion of the conjugate interferes with the initial adhesion and organization of bacteria into biofilms, preventing the stable structured communities from forming. This preliminary prevention is more effective than attempting to eliminate established biofilms

Inventive Principle:

Principle #9Preliminary anti-action

3Object-affected harmful factors

If PEG polymer is conjugated to AMP, then biofilm formation is inhibited, but molecular complexity increases

Engineering Contradiction:

Improvebiofilm formationVSAvoidconjugate structure

Core Design Contradiction:

Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The invention systematically varies parameters of the PEG-AMP conjugate to optimize performance while managing complexity. Specific parameters including PEG molecular weight (1-50 kDa), AMP amino acid sequence, and conjugation ratio are controlled and optimized. This parameter optimization achieves effective biofilm inhibition with well-defined, reproducible conjugate structures

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20230072630A1Compositions including antimicrobial polymer- peptide conjugates and uses thereof

Publication Date: 2023.03.09 UNIVERSITY OF PUERTO RICO

AI summary

Disclosed herein are PEG-maximin H5 peptide conjugates and methods for using the same in the treatment or prevention of biofilms and biofouling.