Underivatized Controlled Pore Glass for Immunoglobulin Aggregate Removal

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Solution Overview

Problem

The downstream processing of immunoglobulins often results in the formation of dimers and oligomers, which lack antigen-binding activity and are difficult to remove, complicating the purification process and requiring additional steps to achieve low-volume, high-concentration solutions for pharmaceutical applications.

Innovation Solution

The use of underivatized controlled pore glass (uCPG) selectively binds dimeric and oligomeric immunoglobulins at pH values between 5 and 7.5, allowing for the recovery of monomeric immunoglobulins with up to 95% efficiency by adsorption and subsequent removal of aggregates through centrifugation or filtration, without altering the protein structure.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional downstream processing steps (affinity chromatography, ion exchange chromatography) are used to purify immunoglobulins, then non-immunoglobulin molecules and contaminants are removed, but dimers and oligomers form and are difficult to remove

Engineering Contradiction:
Improvepurification qualityVSAvoidaggregate formation
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs controlled pore glass (CPG) with specific pore sizes (50-200 nm) to separate monomeric immunoglobulins from aggregated forms. The porous structure allows size-based discrimination where monomers pass through while larger aggregates are retained, effectively removing harmful aggregates without requiring additional purification steps that might induce further aggregation.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The patent utilizes pH gradient changes to control the binding and elution of immunoglobulins on CPG. By adjusting pH from acidic (binding condition) to neutral/alkaline (elution condition), the method selectively elutes monomeric immunoglobulins while retaining aggregates, thereby improving purification quality and reducing aggregate formation in the final product.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If concentration steps are applied to achieve low volumes for economic handling, then storage and handling efficiency improve, but aggregate formation increases

Engineering Contradiction:
Improvesolution concentrationVSAvoidaggregate formation
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The CPG filtration step is integrated into the concentration process, allowing the system to achieve high concentrations while continuously removing aggregates that form during concentration. The porous structure physically separates aggregates from monomers even at high concentrations, preventing the harmful effect of aggregate accumulation.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The patent applies CPG filtration before final concentration steps to pre-remove aggregates. This preliminary action prevents aggregates from forming during subsequent concentration operations, maintaining solution quality even as concentration increases for economic handling and storage.

Inventive Principle:
Principle #10Preliminary action

3Reliability

If additional purification steps are added to remove aggregates, then product quality improves, but process complexity and time increase

Engineering Contradiction:
Improveproduct qualityVSAvoidprocess steps
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines aggregate removal with existing purification steps by integrating CPG filtration into the flow-through mode of ion exchange chromatography. This merging eliminates the need for separate aggregate removal steps, maintaining product quality while avoiding additional process complexity and time consumption.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The CPG material serves multiple functions: it acts as both a filtration medium for aggregate removal and a chromatography support for purification. This multi-functionality allows a single step to achieve both aggregate removal and purification, improving product quality without adding process complexity.

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

4Reliability

If additional purification steps are added to remove aggregates, then product quality improves, but processing time increases

Engineering Contradiction:
Improveproduct qualityVSAvoidprocessing time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent merges aggregate removal with ion exchange chromatography by using CPG as the chromatography support. Aggregates are removed in the flow-through while monomers are retained and eluted, achieving both purification and aggregate removal in a single operation that does not increase processing time.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The method allows aggregates to be rapidly skipped through the CPG column in the flow-through fraction, separating them quickly from monomers. This rapid separation mechanism minimizes processing time while effectively improving product quality by removing aggregates.

Inventive Principle:
Principle #21Skipping (Rushing through)

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 effectively separates monomeric from aggregated immunoglobulins, maintaining the antigen-binding activity of the monomeric form and simplifying the purification process by achieving high yields of monomeric immunoglobulin while minimizing the formation of aggregates during incubation with uCPG.

Implementation Method 1

underivatized controlled pore glass (uCPG) surfaces selectively bind dimeric and oligomeric, i.e. aggregated, immunoglobulin of class G (IgG) present in a solution

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentEP2558492B1Immunoglobulin aggregate removal
Publication Date: 2016.11.16 F HOFFMANN LA ROCHE & CO AG
  • EP2558492B1 patent drawingFigure 1A~1B
  • EP2558492B1 patent drawingFigure 2
  • EP2558492B1 patent drawingFigure 3

AI summary

For the removal of high molecular weight compounds from recombinantly produced polypeptides generally chromatographic methods are employed. It has been found that underivatized controlled pore glass (uCPG) selectively binds high molecular weight compounds present in a solution. The purified polypeptide can be recovered e.g. from the flow through of a chromatography column containing uCPG as chromatography material. It has been found that this effect is pronounced at a pH value of about 4 to 6 in buffered solutions. With approximately 100 m2 to 150 m2 uCPG surface per g of polypeptide almost 80 % to 95 % of the high molecular weight compounds are removed with a yield of 80 % to 90 % of polypeptide.