Formulation of protein-loaded nanoparticles via freeze-drying

Area of Science:

• Nanotechnology
• Pharmaceutical Sciences
• Biotechnology

Background:

• Oral administration of biological drugs faces challenges due to degradation in the gastrointestinal tract.
• Solid dosage forms are crucial for oral delivery but often overlooked in nanotech formulations.
• Developing stable, orally available protein formulations requires innovative strategies.

Purpose of the Study:

• To develop freeze-dried insulin-zinc nanocomplexes for oral administration.
• To enhance resistance to intestinal fluids while maintaining high protein loading.
• To optimize a novel protein formulation strategy for oral delivery.

Main Methods:

• Incorporation of a freeze-drying step using mannitol or sucrose laurate (SLAE).
• Formulation of new insulin-zinc nanocomplexes.
• Characterization of physicochemical properties (particle size, zeta potential, association efficiency).
• In vitro and in vivo assessment of insulin stability and activity.

Main Results:

• Freeze-dried nanocomplexes showed optimal particle size (~100 nm) and zeta potential (~ -15 mV).
• High association efficiency (>90%) and improved colloidal stability were achieved.
• Insulin activity was fully retained throughout the formulation and freeze-drying process.

Conclusions:

• A novel freeze-drying step enhances oral protein formulation stability.
• The developed dry powder enables efficient protein complexation with zinc.
• This strategy optimizes insulin for oral administration, overcoming previous limitations.