Optimized suction patch design for enhanced transbuccal macromolecular drug delivery.

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Pharmacology

Background:

• Peptide drugs offer broad therapeutic potential but face delivery challenges due to oral degradation and large molecular weight, necessitating subcutaneous injections.
• Existing research has not yet yielded a widely accessible, painless platform for peptide drug administration.
• Buccal drug delivery presents an attractive alternative, but requires effective strategies to overcome biological barriers.

Purpose of the Study:

• To optimize an octopus-inspired buccal patch for improved ease of use, scalability, and efficacy in delivering peptide drugs.
• To investigate the impact of patch design, material properties, and formulation parameters on buccal drug delivery performance.
• To evaluate the in vivo bioavailability of peptide drugs delivered via the optimized buccal patch system.

Main Methods:

• Systematic optimization of patch design (surface area, material) and drug matrix formulation (lyophilization).
• Mechanical property assessments and finite element simulations to understand patch behavior.
• Ex vivo experiments and in vivo studies in beagle dogs to evaluate drug permeation and bioavailability.

Main Results:

• An optimized buccal patch with a >9-fold larger effective surface area, made from medical-grade silicone, demonstrated superior performance.
• In vivo studies showed a 14.6% bioavailability for teriparatide and a 9.6-fold increase in semaglutide bioavailability compared to commercial tablets after 30-min application.
• The optimized patch system facilitated efficient buccal administration of macromolecular drugs.

Conclusions:

• Systematic optimization of the octopus-inspired buccal patch technology significantly enhances the non-invasive delivery of peptide drugs.
• This advanced buccal delivery system offers a promising, painless alternative to injections for macromolecular therapeutics.
• The findings support the clinical translation of this simplified and effective non-invasive dosage form for peptide medications.