Abstract：
Low bioavailability of phenolic compounds (phenolics) results in low in vivo bioactivity, thus their co-encapsulation could enhance potential health benefits. In this study, reconstitutable nanoliposomes loaded with phenolics varying in solubility were fabricated using spray drying after stabilized by chitosan (CH) or whey protein (WP). The physicochemical properties, biocompatibility, digestive fate, and bioactivity retention of phenolics in different forms were investigated. The surface charge of nanoliposomes (NL) shifted from -18.7 mV to positive due to conjugation with cationic CH (53.1 mV) and WP (14 mV) after spray drying while it was -26.6 mV for only spray-dried phenolics (SDP). Encapsulation efficiency of the tested phenolics ranged between 64.7 % and 95.1 %. Simulated gastrointestinal digestion/Caco-2 cell model was used to estimate the digestive fate of the phenolics yielding up to 3-fold higher bioaccessibility for encapsulated phenolics compared to their native form, combined or individually. However, the cellular uptake or transepithelial transport of phenolics did not differ significantly among formulations, except trans-resveratrol in WP-NL. On the contrary, the suppressive effect of phenolics on fatty acid induced hepatocellular lipid accumulation was strongly dependent on the encapsulation method, no activity was retained by SDP. These findings suggested that reconstitutable nanoliposomes can improve the absorption of phenolics by facilitating their bioaccessibility and thermal and/or processing stability during spray drying.
摘要：
低生物利用度的酚类化合物（酚类）导致低的体内生物活性，因此，它们的共同封装可以增强潜在的健康益处。在这项研究中,在通过壳聚糖（CH）或乳清蛋白（WP）稳定后，使用喷雾干燥制备了装有溶解度变化的酚类物质的可重构纳米脂质体。物理化学性质，生物相容性，消化命运，并研究了不同形式酚类物质的生物活性保留。由于喷雾干燥后与阳离子CH(53.1mV)和WP(14mV)缀合,纳米脂质体(NL)的表面电荷从-18.7mV移动到正,而仅喷雾干燥的酚类(SDP)的表面电荷为-26.6mV。测试的酚类物质的包封效率介于64.7%和95.1%之间。模拟胃肠道消化/Caco-2细胞模型用于估计酚类的消化命运，与天然形式相比，胶囊化酚类的生物可及性高达3倍。组合或单独。然而,酚类物质的细胞摄取或跨上皮转运在制剂之间没有显著差异,除了WP-NL中的反式白藜芦醇。相反,酚类物质对脂肪酸诱导的肝细胞脂质积累的抑制作用强烈依赖于包封方法，SDP未保留任何活性.这些发现表明,可重构的纳米脂质体可以通过在喷雾干燥期间促进酚类物质的生物可及性和热和/或加工稳定性来改善酚类物质的吸收。
