School of Biological Science and Medical Engineering, State Key Laboratory of Bioelectronics, Southeast University, Nanjing 210096, China.
Food Funct. 2017 Jul 19;8(7):2512-2522. doi: 10.1039/c7fo00439g.
Literature examples of non-aqueous Pickering emulsions stabilized by fat crystals are very rare. Moreover, the applications of rutin are limited due to its low solubility in both water and oils (less than 0.10 mg g and 0.25 mg g, respectively). Thus, herein, we developed an optimum formulation of a non-aqueous self-double-emulsifying delivery system (SDEDS) containing rutin and evaluated its oral bioavailability. The new formulation stabilized by fat crystals (glycerol monostearate, GMS) and nonionic surfactants was prepared via a two-step emulsification process. The presence of a mixture of GMS crystals and nonionic surfactants effectively improves the stability of the emulsions. The non-aqueous SDEDS spontaneously forms oil-in-oil-in-water (O/O/W) double emulsions in the gastrointestinal environment with the inner oil phase mainly containing the active ingredients. It is stable at both 4 °C and 25 °C for 30 days and could enhance the dissolution properties of the active ingredients. Furthermore, the protection of rutin against digestion-mediated precipitation was observed when the formulation contained a high concentration of GMS crystals. The oral absolute bioavailability of rutin obtained from SDEDS (8.62%) is 1.76-fold higher than that of the actives suspension (4.90%). Thus, the non-aqueous SDEDS is an attractive candidate for the encapsulation of water-insoluble and simultaneously oil-insoluble nutrients (such as rutin) and for use in oral delivery applications.
由脂肪晶体稳定的非水相 Pickering 乳液的文献实例非常罕见。此外，由于芦丁在水和油中的溶解度都很低（分别小于 0.10mg/g 和 0.25mg/g），其应用受到限制。因此，本文开发了一种含有芦丁的非水相自乳化双重给药系统（SDEDS）的最佳配方，并评价了其口服生物利用度。由脂肪晶体（甘油单硬脂酸酯，GMS）和非离子表面活性剂稳定的新配方通过两步乳化工艺制备。GMS 晶体和非离子表面活性剂混合物的存在有效地提高了乳液的稳定性。非水 SDEDS 在胃肠道环境中自发形成油包油包水（O/O/W）双重乳液，内油相主要含有活性成分。它在 4°C 和 25°C 下稳定 30 天，可以增强活性成分的溶解性能。此外，当配方中含有高浓度的 GMS 晶体时，芦丁可以防止消化介导的沉淀。从 SDEDS 获得的芦丁的口服绝对生物利用度（8.62%）是活性混悬剂（4.90%）的 1.76 倍。因此，非水 SDEDS 是一种有吸引力的候选物，可用于封装水不溶性和同时油不溶性营养物质（如芦丁），并用于口服给药应用。
