HIV gp140 Vaccine Formulation Stabilization

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Solution Overview

Problem

The stability of trimeric HIV envelope proteins, such as gp140, is not optimal under conditions used for clinical and commercial manufacturing, leading to chemical and physical degradation, and existing formulations are unpredictable in their stability and compatibility with adjuvants and other HIV antigens.

Innovation Solution

An immunogenic composition comprising 0.05 mg/mL to 5 mg/mL of HIV gp140 protein, 2% to 15% sorbitol, 0.01% to 0.05% polysorbate 20, and 5 to 20 mM histidine buffer at a pH of 5.5 to 7.0, with an optional aluminum phosphate adjuvant, which improves stability and allows for long-term storage at refrigerated temperatures.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If trimeric HIV envelope proteins are used as immunogens, then immune response potency is improved, but formulation stability deteriorates under manufacturing conditions

Engineering Contradiction:
Improveimmune response potencyVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by optimizing the formulation composition including specific buffer systems (pH 6.0-7.0), sugar concentrations (5-15% w/v), surfactant types and concentrations (0.01-0.1% w/v), and protein concentrations (0.1-5 mg/mL). These parameter optimizations resolve the contradiction by maintaining trimeric structure stability while preserving immunogenicity, enabling the protein to remain stable under manufacturing and storage conditions without compromising immune response potency

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If HEPES buffer is used in protein formulation, then buffering capacity is improved, but protein stability deteriorates due to hydrogen peroxide generation

Engineering Contradiction:
Improvebuffering capacityVSAvoidprotein stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent extracts HEPES buffer from the formulation to eliminate the harmful effect of hydrogen peroxide generation during manufacturing. The invention replaces HEPES with alternative buffering systems such as phosphate-buffered saline (PBS) or other compatible buffers that provide adequate buffering capacity without generating oxidative stress, thereby resolving the contradiction between ease of operation and protein stability

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces intermediary substances including sugar molecules (such as sucrose, trehalose, or sorbitol at 5-15% w/v) and surfactants (such as polysorbate 20 or polysorbate 80 at 0.01-0.1% w/v) that act as protective mediators. These intermediaries stabilize the trimeric HIV envelope protein structure and protect against degradation, compensating for the removal of HEPES buffer and maintaining overall formulation stability without requiring the problematic buffering system

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of operation

If trimeric HIV envelope proteins are stored under typical conditions, then accessibility for use is improved, but degradation increases due to chemical and physical instability

Engineering Contradiction:
Improveaccessibility for useVSAvoidchemical and physical stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent applies beforehand cushioning by incorporating stabilizing excipients into the formulation before storage. Sugar molecules (5-15% w/v) and surfactants (0.01-0.1% w/v) are included as protective agents that cushion the trimeric HIV envelope protein against chemical and physical degradation during storage and transport. This pre-protection enables the protein to maintain stability under typical storage conditions without requiring extreme measures, thus resolving the contradiction between accessibility and stability

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentEP3471765B1HIV vaccine formulation
Publication Date: 2024.04.24 JANSSEN VACCINES & PREVENTION BV
  • EP3471765B1 patent drawingFigure 1A~1B
  • EP3471765B1 patent drawingFigure 2A~2B
  • EP3471765B1 patent drawingFigure 2C~2D

AI summary

Immunogenic compositions containing a human immunodeficiency virus (HIV) gp140 protein, sorbitol, polysorbate 20, and histidine buffer are described. The described immunogenic compositions are advantageous in that they are stable at refrigerated temperature for extended periods of time, and are compatible with an adjuvant. Also described are methods of using the immunogenic compositions to induce an immune response against an HIV in a subject. The immunogenic compositions can be administered alone, or in combination with one or more additional HIV antigens, or one or more adenovirus vectors encoding the one or more additional HIV antigens.