Polypeptide Stabilization Using Formula I Compounds and Sugars

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Solution Overview

Problem

Current methods for stabilizing polypeptides during storage, such as refrigeration and freeze-drying, are costly and can lead to denaturation, and are not suitable for all biological materials, especially in developing countries where refrigeration is not available, and existing preservation techniques like freeze-drying are time-consuming and stressful for thermosensitive biomaterials.

Innovation Solution

A method involving an aqueous solution of polypeptides with compounds of formula (I) or their physiologically acceptable salts/esters and one or more sugars, which are then dried to form a stable composition, providing thermal resistance and eliminating the need for cold storage, while preserving the polypeptide's activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If refrigeration is used for storage, then polypeptide stability is improved, but storage cost and infrastructure requirements increase

Engineering Contradiction:

Improvepolypeptide stabilityVSAvoidstorage cost

Core Design Contradiction:

ReliabilityVSUse of energy by stationary object

Solution Approach 1:

The invention changes the physical-chemical parameters of the storage system by introducing compounds of formula (I) and sugars that enable stable storage at ambient temperature, eliminating the need for refrigeration and thereby reducing storage costs while maintaining polypeptide stability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

Compounds of formula (I) and sugars act as intermediary stabilizing agents that protect the polypeptide structure during storage, mediating between the polypeptide and environmental stressors to enable stable storage without refrigeration

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If freeze-drying is used for preservation, then shelf life is extended, but the process is time-consuming and can denature proteins

Engineering Contradiction:

Improveshelf lifeVSAvoiddrying time

Core Design Contradiction:

Duration of action of stationary objectVSLoss of time

Solution Approach 1:

The invention applies preliminary protective action by incorporating compounds of formula (I) and sugars into the polypeptide formulation before drying, which pre-protect the protein structure from denaturation stresses during the drying process and enable faster, gentler drying conditions

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The stabilizing compounds modify the physical-chemical parameters of the drying process, allowing for reduced drying time and lower stress conditions while maintaining protein integrity and extending shelf life

Inventive Principle:

Principle #35Parameter changes

3Reliability

If freeze-drying is used, then storage stability is improved, but protein denaturation increases due to freezing and drying stresses

Engineering Contradiction:

Improvestorage stabilityVSAvoidprotein denaturation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Compounds of formula (I) and sugars provide beforehand cushioning by forming a protective matrix around the polypeptide molecules, cushioning them against the harmful effects of freezing and drying stresses before they occur

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Solution Approach 2:

The stabilizing compounds act as intermediary protective layers between the polypeptide and environmental stresses, mediating the interaction and preventing direct damage from freezing and drying conditions

Inventive Principle:

Principle #24Intermediary (Mediator)

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 method effectively maintains polypeptide structure and function during drying, offering improved thermal resistance, extended shelf life, and simplified storage and transport, without requiring a cold chain, and acts as a cryoprotectant, lyoprotectant, and thermoprotectant.

Implementation Method 1

acts as a cryoprotectant, lyoprotectant, and thermoprotectant

Methodology Applied

Scientific EffectCryoprotection:

Implementation Method 2

acts as a cryoprotectant, lyoprotectant, and thermoprotectant

Methodology Applied

Scientific EffectLyoprotection:

Implementation Method 3

acts as a cryoprotectant, lyoprotectant, and thermoprotectant

Methodology Applied

Scientific EffectThermoprotection:

Implementation Method 4

drying the solution to form a composition incorporating the polypeptide

Methodology Applied

Scientific EffectEvaporation: Evaporation

Data Source

PatentUS10029007B2Stabilisation of polypeptides

Publication Date: 2018.07.24 IOSBIO LTD

AI summary

A method for preserving a polypeptide comprising: (a) providing an aqueous solution of (i) the polypeptide, (ii) one or more sugars, and (iii) a compound of formula (I) or a physiologically acceptable salt or ester thereof and/or a compound of formula (II) or a physiologically acceptable salt or ester thereof; and (b) drying the solution to form a composition incorporating the polypeptide.