High-Concentration Antibody Formulation via Solvent-Based Dehydration

Area of Science:

• Biopharmaceutical formulation
• Drug delivery systems
• Materials science

Background:

• Subcutaneous (SC) delivery is preferred for biologics but requires high-concentration antibody formulations.
• High-concentration antibody solutions suffer from instability and high viscosity.
• Existing methods like non-aqueous solutions or hydrogel microparticles have limitations.

Purpose of the Study:

• To develop a new formulation process for high-concentration antibody hydrogel microparticles for SC delivery.
• To achieve antibody concentrations comparable to non-aqueous formulations in an aqueous system.
• To ensure structural and functional stability of antibodies within the microparticles.

Main Methods:

• Antibody concentration and encapsulation into hydrogel microparticles using solvent-based dehydration.
• Continuous microparticle synthesis with simultaneous dehydration and antibody precipitation.
• Analysis of antibody phase behavior and precipitation-dehydration kinetics.

Main Results:

• Developed an aqueous particle suspension with a formulation concentration of 360 mg/mL.
• Antibodies remained structurally and functionally stable post-processing and after 4 months.
• Achieved clinically acceptable injectability with glide force <20 N.

Conclusions:

• Presented the first aqueous antibody formulation at high concentrations suitable for SC administration.
• The novel formulation process overcomes limitations of existing high-concentration delivery methods.
• The process is a potential platform for various SC biologic applications.