Galectin-9 Formulation Buffering for Protein Stability

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Solution Overview

Problem

Existing pharmaceutical formulations for recombinant galectin-9 protein suffer from instability issues, leading to denaturation, oxidation, aggregation, and degradation, which compromise efficacy and may cause adverse effects.

Innovation Solution

A pharmaceutical formulation comprising recombinant stabilized galectin-9 protein, a buffer, and a stabilizer, specifically using histidine acetate buffer and stabilizers like trehalose and mannitol, to enhance stability and maintain carbohydrate recognition activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Device complexity

If recombinant galectin-9 protein is formulated without sufficient stabilizers, then formulation complexity is reduced, but the protein stability deteriorates leading to denaturation, oxidation, aggregation, and degradation

Engineering Contradiction:
Improveformulation complexityVSAvoidprotein stability
Core Design Contradiction:
Device complexityVSStability of the object's composition

Solution Approach 1:

The formulation employs a composite stabilizer system combining multiple excipients (sugars, amino acids, surfactants, and buffers) that work synergistically to protect the galectin-9 protein. This composite approach addresses the contradiction by distributing the stabilization function across multiple components rather than relying on a single complex agent, thereby maintaining protein stability while managing formulation complexity.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The formulation optimizes specific parameters including pH (using histidine acetate buffer), ionic strength, and excipient concentrations to create an environment that inherently stabilizes the protein. By adjusting these physical-chemical parameters, the formulation reduces protein instability without requiring excessively complex stabilizer combinations.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If stabilizer concentration is increased to improve protein stability, then protein stability is enhanced, but the formulation may exhibit adverse effects such as toxicity

Engineering Contradiction:
Improveprotein stabilityVSAvoidadverse effects
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The formulation carefully optimizes excipient concentrations within safe pharmacological ranges. For example, sugars and amino acids are used at concentrations that provide adequate stabilization while remaining below toxicity thresholds. This parameter optimization allows the formulation to achieve necessary protein stability without introducing harmful effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The formulation uses multiple excipients as intermediary protective agents that indirectly stabilize the protein through various mechanisms (osmotic pressure, hydrogen bonding, micelle formation) rather than relying on high concentrations of a single potent stabilizer that might be toxic. This distributed intermediary approach reduces adverse effects while maintaining stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If buffer system is optimized to maintain pH for protein stability, then protein stability is improved, but formulation complexity increases due to multiple buffer components

Engineering Contradiction:
Improveprotein stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The histidine acetate buffer system performs multiple functions simultaneously: it maintains optimal pH for galectin-9 stability, provides ionic strength control, and contributes to overall formulation buffering capacity. This multi-functionality reduces the need for separate pH control agents, thereby managing formulation complexity while ensuring protein stability.

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

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 formulation provides enhanced stability and efficacy of recombinant galectin-9 protein, maintaining its biological activity and reducing adverse effects, suitable for the prevention or treatment of bone diseases and cancers.

Implementation Method 1

a buffer; and b. a stabilizer

Methodology Applied
Scientific EffectBuffering:

Implementation Method 2

a pharmaceutical formulation in which galectin-9 protein is stably preserved through combination with a buffer and a stabilizer

Methodology Applied
Scientific EffectStabilization:

Data Source

PatentEP4663183A1Stabilized formulation comprising recombinant stabilized galectin 9 protein
Publication Date: 2025.12.17 GBIOLOGICS INC
  • EP4663183A1 patent drawingFigure 1~2
  • EP4663183A1 patent drawingFigure 3~4a
  • EP4663183A1 patent drawingFigure 4b~4c

AI summary

The present invention relates to a stabilized pharmaceutical formulation comprising a recombinant stabilized galectin-9 protein. More specifically, the invention provides a pharmaceutical formulation with improved stability through the combination of a buffer and a stabilizer.