Sequence-Controlled Delivery of Peptides from Hierarchically Structured Nanomaterials

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Nanotechnology

Background:

• Peptide drugs often degrade in the gastrointestinal tract, limiting oral bioavailability.
• Effective oral delivery systems are needed to protect peptides and ensure therapeutic function.

Purpose of the Study:

• To develop a hierarchically structured, pH-responsive drug delivery system for oral peptide administration.
• To create a nanoparticle-in-nanofiber configuration capable of sequential, stimuli-triggered release.

Main Methods:

• Encapsulation of a model peptide within pH-responsive nanoparticles under mild conditions.
• Electrospinning of nanoparticles with a pH-responsive mucoadhesive polymer to form nanofibers.
• Characterization of nanoparticle release from nanofibers and peptide release from nanoparticles in response to pH changes.

Main Results:

• A hierarchical nanoparticle-in-nanofiber system was successfully fabricated.
• The system demonstrated pH-responsive release of nanoparticles and subsequently encapsulated peptides.
• Nanoparticles showed compatibility with Caco-2 cells, with endocytosis mechanisms elucidated.

Conclusions:

• The developed hierarchical system offers a promising strategy for oral peptide drug delivery.
• pH-responsive and sequential release mechanisms enhance drug protection and bioavailability.
• The biocompatibility and cellular interaction of the nanoparticles support their potential therapeutic application.