Development, Characterization, and in vitro Efficacy Evaluation of an Inhalable H1B Antimicrobial Peptide Formulation...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Biochemistry

Background:

• Hymenochirin-1B (H1B), an antimicrobial peptide from frog secretions, exhibits anticancer properties against non-small cell lung cancer (NSCLC).
• Stabilizing H1B is crucial for developing effective inhalation therapies for NSCLC.

Purpose of the Study:

• To formulate Hymenochirin-1B (H1B) into a stable, inhalable dry powder (H1BSD) for non-small cell lung cancer (NSCLC) treatment.
• To characterize the physical properties, aerosolization performance, and stability of the H1BSD formulations.

Main Methods:

• Spray drying of H1B with excipients (mannitol, trehalose, L-leucine) to create H1BSD powders.
• Characterization using DSC, PXRD, and aerodynamic particle sizing.
• In vitro efficacy and stability studies at 25°C for 3 months.

Main Results:

• All H1BSD powders showed high yield, drug content (~100%), low moisture (<3%), and optimal aerodynamic properties for inhalation.
• The optimal formulation (H1BSD4) demonstrated therapeutic efficacy in vitro.
• Formulations H1BSD2-H1BSD5 remained stable for 3 months, retaining >90% drug content and semi-crystalline structure.

Conclusions:

• Successfully developed a stable, inhalable dry powder formulation (H1BSD) of Hymenochirin-1B (H1B).
• The H1BSD formulation maintains anticancer activity and offers enhanced stability and optimized inhalation delivery for NSCLC treatment.