Meningococcus Serogroup X Conjugate Vaccine Stability

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Solution Overview

Problem

Current vaccines against Neisseria meningitidis serogroup X are ineffective due to the instability of its capsular polysaccharides in aqueous solutions and lack of immunogenicity, requiring refrigeration and inadequate quantification methods, which hinder the development of a stable and immunogenic vaccine.

Innovation Solution

Conjugation of serogroup X capsular polysaccharides to carrier molecules using direct coupling methods, such as oxidizing primary hydroxyl groups and reductive amination, to create stable conjugates suitable for aqueous formulations, and the use of HPAEC-PAD for selective quantification.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If polysaccharides are presented in lyophilized form to improve stability, then stability is improved, but convenience and ease of operation deteriorate due to requiring reconstitution and cold storage

Engineering Contradiction:
ImprovestabilityVSAvoidconvenience
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The patent changes the chemical parameters of the polysaccharide by conjugating it to carrier proteins (such as tetanus toxoid or CRM197). This chemical modification fundamentally alters the stability properties of the polysaccharide, enabling it to remain stable in aqueous solution without requiring lyophilization or cold storage, thus resolving the contradiction between stability and convenience

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite materials by conjugating the polysaccharide with carrier proteins to form glycoconjugates. This composite structure combines the immunogenic properties of the protein carrier with the antigenic properties of the polysaccharide, while simultaneously providing enhanced stability in aqueous formulations without requiring refrigeration

Inventive Principle:
Principle #40Composite materials

2Reliability

If polysaccharides are conjugated to carrier molecules, then immunogenicity is improved, but manufacturing complexity worsens due to additional conjugation steps

Engineering Contradiction:
ImproveimmunogenicityVSAvoidmanufacturing complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses carrier proteins as intermediary molecules that facilitate the conversion of T-independent polysaccharide antigens into T-dependent glycoconjugate vaccines. The carrier protein acts as a mediator that not only enhances immunogenicity but also provides a standardized platform for conjugation, actually simplifying the overall manufacturing process by using well-established protein chemistry techniques

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs universal carrier proteins (such as tetanus toxoid or CRM197) that can serve multiple functions: enhancing immunogenicity, providing a standardized conjugation platform, and enabling the development of multivalent vaccines. This multi-functionality reduces manufacturing complexity by using the same carrier system across different vaccine formulations

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

3Difficulty of detecting and measuring

If standard quantification methods are used for polysaccharides, then measurement simplicity is improved, but measurement precision deteriorates due to inability to distinguish polysaccharide from degradation products

Engineering Contradiction:
Improvemeasurement simplicityVSAvoidmeasurement precision
Core Design Contradiction:
Difficulty of detecting and measuringVSMeasurement precision

Solution Approach 1:

The patent replaces conventional mechanical/chemical quantification methods (such as phenol-sulfuric acid assay) with high-performance anion-exchange chromatography with pulsed amperometric detection (HPAEC-PAD). This substitution uses electrochemical detection principles to specifically identify and quantify polysaccharide based on its unique phosphate group signature, achieving both precision and automation

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The HPAEC-PAD method provides real-time feedback through characteristic elution profiles and amperometric signals that specifically identify polysaccharide versus degradation products. The system continuously monitors and quantifies the polysaccharide based on its unique electrochemical properties, enabling precise measurement without ambiguity

Inventive Principle:
Principle #23Feedback

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 resulting conjugates are immunogenic, stable in aqueous solutions, and can be used in vaccines without refrigeration, providing effective protection against serogroup X meningococcal disease while allowing for precise quantification.

Implementation Method 1

oxidizing primary hydroxyl groups

Methodology Applied
Scientific EffectOxidation: Oxidation

Implementation Method 2

reductive amination

Methodology Applied
Scientific EffectReductive amination: Redox Reactions

Implementation Method 3

HPAEC-PAD

Methodology Applied
Scientific EffectIon exchange chromatography: Ion Exchange

Implementation Method 4

HPAEC-PAD

Methodology Applied
Scientific EffectPulsed amperometric detection:

Data Source

PatentEP2852414B9Meningococcus serogroup x conjugate
Publication Date: 2020.12.09 GLAXOSMITHKLINE BIOLOGICALS SA
  • EP2852414B9 patent drawingFigure 1
  • EP2852414B9 patent drawingFigure 2
  • EP2852414B9 patent drawingFigure 3

AI summary

The invention provides a conjugate of a Neisseria meningitidis serogroup X capsular polysaccharide and a carrier molecule. The conjugate is typically made by (a) oxidising a primary hydroxyl group in the capsular polysaccharide, to give an oxidised polysaccharide with an aldehyde group; and (b) coupling the oxidised polysaccharide to a carrier molecule via the aldehyde group, thereby giving the conjugate. The conjugate may be part of an immunogenic composition. This composition may comprise one or more further antigens, particularly capsular polysaccharides from serogroups A, W135, C and Y and conjugated forms thereof. The composition may be in an aqueous formulation. The composition is useful as a vaccine, e.g. for raising an immune response in a mammal. The invention also provides processes for making the conjugate.