Recombinant G-CSF Refolding and Purification Process

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current methods for producing recombinant human G-CSF from inclusion bodies are time-consuming, labor-intensive, and costly, with previous processes involving energy-consuming cooling and resulting in significant protein yield loss, and lack efficient purification to remove conformational isoforms.

Innovation Solution

A method involving solubilization of G-CSF with a denaturing agent and reducing agent, followed by refolding in a redox system at moderate temperatures, and subsequent purification using reversed phase chromatography preceded by cation exchange chromatography, allowing for efficient renaturation and purification within a shorter timeframe without energy-intensive cooling.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If refolding is performed at low temperatures for more than half a day, then protein renaturation efficiency is improved, but energy consumption increases and production time extends

Engineering Contradiction:
Improveprotein renaturation efficiencyVSAvoidenergy consumption
Core Design Contradiction:
ReliabilityVSUse of energy by stationary object

Solution Approach 1:

The patent changes the temperature parameter from low temperature (4°C) to moderate temperature (20-37°C) and adjusts the refolding time parameter from more than half a day to several hours, achieving both energy savings and maintained renaturation efficiency through optimized parameter combination

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent performs preliminary solubilization of inclusion bodies using denaturants and reducing agents before refolding, which prepares the protein for faster refolding at moderate temperatures, reducing the overall process time and energy requirements

Inventive Principle:
Principle #10Preliminary action

2Quantity of substance

If traditional purification methods are used, then protein yield is maintained, but purification efficiency is low and conformational isoforms are not effectively removed

Engineering Contradiction:
Improveprotein yieldVSAvoidpurification efficiency
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The patent uses refolding conditions with oxidized and reduced glutathione as intermediaries to promote proper disulfide bond formation, which enables effective separation of correctly folded protein from conformational isoforms during subsequent purification, achieving both high yield and high purity

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent optimizes purification parameters including pH, ionic strength, and temperature to enhance the separation efficiency between correctly folded G-CSF and conformational isoforms, improving both purification speed and effectiveness

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If multiple chromatography steps are performed, then purification purity is improved, but process complexity and time consumption increase

Engineering Contradiction:
Improvepurification purityVSAvoidprocess complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent combines solubilization, refolding, and purification into an integrated process where refolding conditions are optimized to simultaneously promote proper folding and enable effective separation from impurities, reducing the need for multiple separate purification steps

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent maintains continuous useful action by performing refolding and purification in a streamlined sequence without intermediate storage or processing steps, keeping the protein in active folding conditions throughout the process to maintain high purity while reducing overall process time

Inventive Principle:
Principle #20Continuity of useful action

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

This method achieves a highly purified and homogeneous G-CSF preparation with minimal loss of protein yield, effectively removing conformational isoforms and reducing production time and costs, resulting in a product suitable for therapeutic use with improved pharmacokinetic and pharmacodynamic properties.

Implementation Method 1

refolding the G-CSF by diluting the solubilizate with a refolding buffer containing reduced and oxidized glutathione

Methodology Applied
Scientific EffectRedox reactions: Redox Reactions

Implementation Method 2

purifying the refolded G-CSF by at least one chromatography step comprising reversed phase (RP) chromatography, preceded by a cation exchange (CEX) chromatography

Methodology Applied
Scientific EffectIon exchange: Ion Exchange

Implementation Method 3

at least one chromatography step comprised a reversed phase (RP) chromatography

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Data Source

PatentEP2547699B1Method for obtaining biologically active recombinant human g-csf
Publication Date: 2016.10.19 RATIOPHARM GMBH
  • EP2547699B1 patent drawingFigure 1
  • EP2547699B1 patent drawingFigure 2
  • EP2547699B1 patent drawingFigure 3A~3B

AI summary

Provided is a method of obtaining biologically active recombinant human G-CSF from inclusion bodies, wherein the solubilization and refolding process can be performed at ambient temperature and the purification step comprises reversed phase chromatography (RP), in particular RP-HPLC. The G-CSF preparation so obtained is characterized by high purity and homogeneity.