Regulation of the colon-targeted release rate of lactoferrin by constructing hydrophobic ethyl cellulose/pectin composite nanofibrous carrier and its effect on anti-colon cancer activity.

In order to modify colonic release behavior of lactoferrin (Lf), a hydrophobic composite nanofibrous carrier (CNC) was constructed by emulsion coaxial electrospinning. Ethylcellulose/pectin based water-in-oil emulsion and Lf-contained polyvinyl alcohol solution were used as shell and core fluids, respectively. An electrospinning diagram was first constructed to screen out suitable viscosity (51–82 cP) and conductivity (960–1300 μS/cm) of the dispersed phase of pectin solution for successful electrospinning of shell emulsion. Varying mass fraction of pectin solution (5 %–20 %) of shell emulsion during emulsion coaxial electrospinning obtained CNCs with different micro-structures, labeled as 5&95 CNC, 10&90 CNC, 15&85 CNC, 20&80 CNC. These CNCs all achieved colonic delivery of Lf (>95 %), and the time for complete release of Lf in simulated colon fermentation process were 10, 7, 5 and 3 h, respectively. That is, the greater the pectin content in CNC, the faster the release rate of stabilized Lf in colon. Lf release in simulated colon fermentation fluid involved complex mechanisms, in which diffusion release of Lf was dominant. Increasing colonic release rate of Lf enhanced its regulation effect on the expression levels of cell cycle arrest and apoptosis-related protein and promote its effective inhibition on the proliferation of HCT116 cell. • Composite nanofibrous carrier (CNC) was fabricated by emulsion coaxial electrospinning. • CNC involved hydrophobic outer layer, ethylcellulose-pectin middle layer, and core of Lf. • CNC with various microstructure was obtained by varying mass fraction of pectin solution. • The greater the pectin content in CNC, the faster the release rate of stabilized Lf in colon. • Faster rate of Lf release generated higher anti-proliferation activity against HCT116 cells. [ABSTRACT FROM AUTHOR]