Blueberry anthocyanin(BA)have attracted much attention for their diverse bioactivities,but their practical useis greatly limited by poor stability and low bioavailability.The complex intestinal environment causes them...Blueberry anthocyanin(BA)have attracted much attention for their diverse bioactivities,but their practical useis greatly limited by poor stability and low bioavailability.The complex intestinal environment causes them todegrade extensively,significantly reducing their absorption efficiency.To address this,the present study focuseson the sublingual delivery route,aiming to enhance the bioavailability of anthocyanins by reducing the hepaticfirst-pass effect.In this research,macromolecules such as polyvinyl alcohol(PVA),gelatin(GEL),and pullulan(PUL)were used as carriers to load anthocyanins.Through electrospinning,anthocyanin-loaded oral dissolvingfilms(ODF)were successfully prepared,which can be used for the sublingual delivery of anthocyanins.Experimentsconfirmed that the mechanical properties of the fiber membrane reached an optimal state when the massfractions of PVA,GEL,and PUL were 8,10 and 11%respectively.Characterization results from scanning electronmicroscopy(SEM),Fourier transform infrared spectroscopy(FTIR),and X-ray diffraction(XRD)revealed thatintermolecular hydrogen bonds were formed in the system,strengthening intermolecular interactions.Moreover,BA maintained good stability at 312.96℃.Simulated oral release experiments demonstrated that the PGPmembrane containing 10%BA achieved a release rate of 82%within 10 min,following a near-Fickian diffusionmechanism.Cytotoxicity tests confirmed the good biosafety of the material,and porcine mucosal permeationstudies indicated that BA could be released through the oral mucosa.This study provides a new carrier designand theoretical support for the oral delivery of anthocyanins.展开更多
基金supported by the National Key R&D Program of China(2024YFD1600604).
文摘Blueberry anthocyanin(BA)have attracted much attention for their diverse bioactivities,but their practical useis greatly limited by poor stability and low bioavailability.The complex intestinal environment causes them todegrade extensively,significantly reducing their absorption efficiency.To address this,the present study focuseson the sublingual delivery route,aiming to enhance the bioavailability of anthocyanins by reducing the hepaticfirst-pass effect.In this research,macromolecules such as polyvinyl alcohol(PVA),gelatin(GEL),and pullulan(PUL)were used as carriers to load anthocyanins.Through electrospinning,anthocyanin-loaded oral dissolvingfilms(ODF)were successfully prepared,which can be used for the sublingual delivery of anthocyanins.Experimentsconfirmed that the mechanical properties of the fiber membrane reached an optimal state when the massfractions of PVA,GEL,and PUL were 8,10 and 11%respectively.Characterization results from scanning electronmicroscopy(SEM),Fourier transform infrared spectroscopy(FTIR),and X-ray diffraction(XRD)revealed thatintermolecular hydrogen bonds were formed in the system,strengthening intermolecular interactions.Moreover,BA maintained good stability at 312.96℃.Simulated oral release experiments demonstrated that the PGPmembrane containing 10%BA achieved a release rate of 82%within 10 min,following a near-Fickian diffusionmechanism.Cytotoxicity tests confirmed the good biosafety of the material,and porcine mucosal permeationstudies indicated that BA could be released through the oral mucosa.This study provides a new carrier designand theoretical support for the oral delivery of anthocyanins.