摘要
Overcoming gastrointestinal tract barriers to enhance bioavailability is a major challenge for oral delivery. The innovative design of multi-compartment functional Pickering emulsions would provide an ideal option for targeted co-delivery of bioactive components. In this study, pH-responsive water-in-oil-in-water (W/O/W) Pickering double emulsions co-loaded with curcumin and fluorouracil were fabricated by zein/anthocyanin (ACN)/Zn 2+ nanoparticles (ZAZn NPs) via a one-step emulsification process. The unique emulsifier was designed by depositing ACN-Zn 2+ complexes on zein nanoparticles (zein NPs). The binding of ACN to the nanoparticle surface through hydrogen bonding interaction enhanced the hydrophilization and stimuli-response of zein NPs. Furthermore, the co-ordination of Zn 2+ and ACN facilitated the formation of nanoparticles with near-neutral wettability, which served as the dominant driving force for the one-step generation of W/O/W Pickering emulsions. The droplet size, distribution and internal structure of Pickering double emulsions were influenced by nanoparticle concentration and oil fraction. Due to Zn 2+ complexation with curcumin at the oil/water interface, the W/O/W Pickering emulsions obtained exhibited high curcumin encapsulation efficiency (91.2%) and free fatty acid release degree (65.9%), resulting in increased bio-accessibility (71.0%). The simulated gastrointestinal release demonstrated that curcumin and fluorouracil achieved controlled intestinal release, which was driven by a pH-mediated competitive adsorption-desorption mechanism. Moreover, in vitro cell experiments showed that co-encapsulated Pickering double emulsions exhibited 2.5 times greater bio-activity than those containing fluorouracil only. This facile strategy for preparing Pickering double emulsions is promising for the co-delivery of different physico-chemical bio-active compounds, which would improve oral bio-accessibility and bio-activity.
危险品化学品经营许可证（带存储）