Stabilization and Transdermal Delivery of an Investigational Peptide Using MicroCor® Solid-State Dissolving...

Area of Science:

• Biopharmaceutical formulation
• Drug delivery systems
• Transdermal drug delivery

Background:

• Biotherapeutics often face stability challenges, necessitating refrigerated storage.
• Peptide A, a developmental compound, exhibited poor stability in liquid formulations for subcutaneous injection.

Purpose of the Study:

• To assess the feasibility of formulating Peptide A in MicroCor® microstructure arrays (MSAs) for transdermal delivery.
• To evaluate the stability and bioavailability of Peptide A delivered via MSAs.

Main Methods:

• A 5600-needle MSA (2 cm², ~200 μm microstructures) was loaded with a therapeutic dose of Peptide A.
• Stability of the Peptide A-loaded MSAs was assessed under room-temperature storage for 3 months.
• In vivo studies were conducted on Yucatan minipigs to evaluate skin irritation, peptide transfer efficiency, and absolute bioavailability.

Main Results:

• Peptide A-loaded MSAs demonstrated stability at room temperature for 3 months.
• Transdermal delivery via MSAs resulted in mild and transient skin irritation in minipigs.
• High peptide transfer efficiency was observed, yielding an absolute bioavailability of 74%, comparable to subcutaneous injection (73%).

Conclusions:

• MicroCor® technology provides a viable alternative for delivering Peptide A, overcoming its inherent stability issues.
• Transdermal delivery using MSAs significantly enhances the stability of Peptide A compared to liquid formulations.
• This approach offers a promising strategy for stable and effective delivery of challenging peptide therapeutics.