National R&D Center of Freshwater Fish Processing, College of Life Science, Jiangxi Normal University, Nanchang, Jiangxi 330022, China.
National R&D Center of Freshwater Fish Processing, College of Life Science, Jiangxi Normal University, Nanchang, Jiangxi 330022, China; Jiangxi Deshang Pharmaceutical Co., Ltd., Yichun, Jiangxi 330006, China.
Int J Biol Macromol. 2023 Dec 31;253(Pt 7):127554. doi: 10.1016/j.ijbiomac.2023.127554. Epub 2023 Oct 20.
Urolithin A (UroA) is gut metabolites of ellagitannins possessing a vast range of biological activities, but its poor water solubility and low bioavailability hinder its potential applications. This study utilized the pH dependent dissolution characteristics of UroA and employed a simple pH-driven method to load UroA into liposomes. The characterization and stability of obtained liposomes under different conditions were evaluated, and their oral bioavailability was tested by pharmacokinetics, and compared with UroA liposomes prepared using traditional thin film dispersion (TFM-ULs). Results indicated that liposomes could effectively encapsulate UroA. The UroA liposomes prepared by the pH-driven method (PDM-ULs) showed lower particle size, polydispersity index, zeta potential, and higher encapsulation efficiency than TFM-ULs. Interestingly, better thermal stability, storage stability, in vitro digestion stability, and higher bioaccessibility were also found on PDM-ULs. Moreover, pharmacokinetic experiments in rats demonstrated that PDM-ULs could significantly improve the bioavailability of UroA, with an absorption efficiency 1.91 times that of TFM-ULs. Therefore, our findings suggest that liposomes prepared by pH-driven methods have great potential in improving the stability and bioavailability of UroA.
尿石素 A（UroA）是鞣花单宁的肠道代谢物，具有广泛的生物学活性，但由于其水溶性差和生物利用度低，限制了其潜在应用。本研究利用 UroA 的 pH 依赖性溶解特性，采用简单的 pH 驱动方法将 UroA 载入脂质体。评估了不同条件下所得脂质体的特性和稳定性，并通过药代动力学测试比较了其口服生物利用度与采用传统薄膜分散法（TFM-ULs）制备的 UroA 脂质体。结果表明，脂质体可以有效地包封 UroA。与 TFM-ULs 相比，pH 驱动法（PDM-ULs）制备的 UroA 脂质体具有更小的粒径、更低的多分散指数、更高的zeta 电位和更高的包封效率。有趣的是，PDM-ULs 还具有更好的热稳定性、储存稳定性、体外消化稳定性和更高的生物利用度。此外，大鼠的药代动力学实验表明，PDM-ULs 可显著提高 UroA 的生物利用度，其吸收效率是 TFM-ULs 的 1.91 倍。因此，我们的研究结果表明，pH 驱动法制备的脂质体在提高 UroA 的稳定性和生物利用度方面具有很大的潜力。
