尿石素A(UroA)是具有广泛生物活性的eligagannins的肠道代谢产物,但其水溶性差和生物利用度低阻碍了其潜在的应用。这项研究利用了UroA的pH依赖性溶出特性,并采用了一种简单的pH驱动方法将UroA加载到脂质体中。对所获得的脂质体在不同条件下的表征和稳定性进行了评价,通过药代动力学测试了它们的口服生物利用度,并与使用传统薄膜分散体(TFM-ULs)制备的UroA脂质体进行了比较。结果表明脂质体可以有效地包封UroA。通过pH驱动方法(PDM-ULs)制备的UroA脂质体显示出较低的粒径,多分散指数,zeta电位,和比TFM-ULs更高的封装效率。有趣的是,更好的热稳定性,储存稳定性,体外消化稳定性,在PDM-ULs上也发现了更高的生物可及性。此外,在大鼠体内的药代动力学实验表明,PDM-ULs可以显着提高UroA的生物利用度,吸收效率是TFM-ULs的1.91倍。因此,我们的研究结果表明,通过pH驱动方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巨大潜力.
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.