Surfactant-Modified Peptides for Prolonged Action and Stability

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Solution Overview

Problem

Peptide and protein-based therapeutics face limitations such as short duration of action, poor bioavailability, instability, and lack of receptor subtype selectivity, along with issues like aggregation that can lead to immunological responses.

Innovation Solution

Covalently modifying peptides and proteins with surfactants like alkyl glycosides to enhance stability, bioavailability, selectivity, and duration of action, by attaching hydrophilic and hydrophobic groups via linker amino acids, forming surfactant-modified peptides with improved pharmaceutical properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If peptides and proteins are used as therapeutics, then therapeutic effects are achieved, but stability and duration of action are limited

Engineering Contradiction:
Improveduration of actionVSAvoidstability
Core Design Contradiction:
Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent applies composite materials by conjugating peptides or proteins with surfactant molecules to create a composite therapeutic agent. This composite structure combines the biological activity of the peptide/protein with the stabilizing and prolonging properties of the surfactant, thereby simultaneously improving both stability and duration of action

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent employs parameter changes by modifying the physical and chemical properties of peptides and proteins through covalent attachment of surfactants. This changes parameters such as hydrophobicity, molecular weight, and solubility, which directly influence stability and pharmacokinetic behavior, leading to extended duration of action

Inventive Principle:
Principle #35Parameter changes

2Reliability

If peptides and proteins are administered, then therapeutic effects are achieved, but bioavailability is poor

Engineering Contradiction:
ImprovebioavailabilityVSAvoidcomplexity of modification
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses surfactant molecules as intermediaries to improve the bioavailability of peptides and proteins. The surfactant acts as a mediator that facilitates better distribution, solubility, and cellular uptake of the therapeutic peptide or protein, thereby enhancing its bioavailability without requiring complex delivery systems

Inventive Principle:
Principle #24Intermediary (Mediator)

3Object-affected harmful factors

If peptides and proteins are used, then therapeutic effects are achieved, but aggregation occurs leading to immunological responses

Engineering Contradiction:
ImproveimmunogenicityVSAvoidaggregation
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent converts the potentially harmful aggregation tendency of peptides and proteins into a beneficial effect by using surfactant conjugation. The surfactant prevents unwanted aggregation while the controlled aggregation or depot formation at the injection site prolongs release, thereby reducing immunogenicity while extending duration of action

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 covalent modification of peptides and proteins with surfactants results in improved stability, bioavailability, and receptor selectivity, reducing aggregation and immunogenicity, leading to prolonged pharmacokinetic behavior and enhanced therapeutic effects.

Implementation Method 1

Covalently modified peptide and protein analogs allow for improved pharmaceutical properties

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Implementation Method 2

covalently modified peptides and/or proteins are attached to glycoside surfactants

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Data Source

PatentEP4047023A1Improved peptide pharmaceuticals
Publication Date: 2022.08.24 EUMEDERIS PHARMACEUTICALS INC
  • EP4047023A1 patent drawingFigure 1
  • EP4047023A1 patent drawingFigure 1
  • EP4047023A1 patent drawingFigure 1

AI summary

Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.