Bioinspired butyrate-coated tiny carriers for targeted oral delivery of large biological drugs

Butyrate-functionalized nanoparticles demonstrated 2.87-fold higher oral bioavailability compared to bare polyethylene glycol nanoparticles.

• Ligand-functionalization of nanoparticles can enhance their affinity for targeted cells.
• Mucus networks and enzyme deactivation pose challenges for the effectiveness of macromolecular ligands in oral administration.
• Butyrate, a microbiota metabolite, was anchored to polyethylene glycol nanoparticles to improve their targeting efficiency.
• In vitro and in vivo tests showed that butyrate did not impair the mucus permeability or distribution of the nanoparticles.
• Specific interactions between butyrate and the monocarboxylate transporter on cell membranes improved cellular uptake and intestinal absorption.
• Safety assessments indicated that butyrate modification of nanoparticles is non-toxic.

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