Preparation, characterization and evaluation of liposomal-freeze dried anthocyanin-enriched Vaccinium arctostaphylos L. fruit extract incorporated into fast dissolving oral films

Abstract

Anthocyanins are pigments in the polyphenol class, which are found in high amounts especially in dark colored fruits and have high antioxidant properties, but Vaccinium fruit extract has low oral bioavailability and chemical instability. The purpose of this study was to develop a fast dissolving orodispersible film (FDOF) formulation containing anthocyanin-enriched Vaccinium arctostaphylos L. fruit extract and to exploit and evaluate the physical and phytochemical parameters of the formulation. For this purpose, a crude EtOH extract was prepared from the fresh fruits of V. arctostaphylos and the extract was enriched with anthocyanins using column chromatography. The first freeze-dried Vaccinium fruit extract (FVE) was entrapped in liposomal carrier to improve the solubility and stability of the extract, and second, this liposomal dispersion was formulated as FDOFs in order to improve patient compliance. Physical properties such as fragmentation, tensile strength, Young's modulus and elongation at break, FTIR were investigated. Furthermore, the total phenol, flavonoid, anthocyanin content as well as the in vitro antioxidant activity of the F11, F13 formulations were evaluated. The results showed that F6 formulation exploit the best physicomechanical properties z-average 101.3 nm, PDI 0.28, zeta potential −31.9 mV and encapsulation efficiency 91.4% and was used for further studies. The incorporation of FVE to the liposomes and FVE into the films promoted reduction of the tensile strength and Young's modulus, and an increase in elongation. The higher in vitro release data was obtained in F13 than F11 formulation, the film exhibited maximal release in 10 min of the anthocyanin and it was more than 98%. The results indicated that the oral dissolving film formulation loaded with liposomal V. arctostaphylos fruit extract may be a useful and effective antioxidant-containing product with future in vivo studies.