Abstract

Lactoferrin (Lf) is a bioactive protein with varied biological effects. To improve its anti-digestive stability in oral administration, a novel nanocarrier with high hydrophobicity for colonic delivery of Lf was creatively developed by modified coaxial electrospinning. First, a suitable biocompatible solvent, acetic acid, was screened as the mono-solvent for ES100 electrospinning, creating highly-hydrophobic ES100 nanofiber mat (contact angle = 133.8o). Then, Lf-loaded W/O emulsion was prepared as the core fluid to ensure the successful coaxial electrospinning and generate Lf encapsulated core/shell nanofiber mat (ES@Lf). Lf was demonstrated maintaining structural integrity and anti-colon cancer activity during encapsulation and oral delivery. In vitro assay indicated 92.3% Lf was sustainably released in colon, and its release followed a complex mechanism in which the erosion was dominant. Instead of pH-dependent erosion, the synergistic action through gut microbiota adhesion and their metabolites, especially short-chain fatty acids, was illustrated for disintegration of ES@Lf nanofiber for the first time.

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