Argenziano Monica, Ansari Irfan Aamer, Muntoni Elisabetta, Spagnolo Rita, Scomparin Anna, Cavalli Roberta
Department of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, Italy.
Antioxidants (Basel). 2022 May 20;11(5):1007. doi: 10.3390/antiox11051007.
-resveratrol, a polyphenolic phytoalexin found in various plant sources, has been the focus of increasing attention in recent years because of its role in the prevention of many human diseases, and particularly because of its antioxidant properties. However, the in vivo effect of -resveratrol after oral administration is negligible when compared to its efficacy in vitro, due to its low bioavailability. Moreover, it presents stability issues as it is an extremely photosensitive compound when exposed to light. This work aims to develop lipid-coated nanocrystals in order to improve the antioxidant activity and bioavailability of -resveratrol. Lipid-coated -resveratrol nanocrystals with sizes lower than 500 nm, spherical shapes and smooth surfaces were obtained via a milling method. They showed a faster dissolution rate than the coarse -resveratrol powder. The antioxidant properties of -resveratrol were not impaired by the milling process. The in vivo pharmacokinetics of lipid-coated -resveratrol nanocrystals were evaluated after oral administration to rats, with a commercial Phytosome formulation being used for comparison purposes. An increase in the -resveratrol area under the curve was observed and the lipid-coated nanocrystal formulation led to an enhancement in the oral bioavailability of the compound.
白藜芦醇是一种存在于多种植物来源中的多酚类植物抗毒素，近年来因其在预防多种人类疾病中的作用，特别是因其抗氧化特性而受到越来越多的关注。然而，与体外疗效相比，白藜芦醇口服后的体内效果可忽略不计，这是由于其生物利用度低。此外，由于它在光照下是一种极其光敏的化合物，所以存在稳定性问题。这项工作旨在开发脂质包衣纳米晶体，以提高白藜芦醇的抗氧化活性和生物利用度。通过研磨法获得了尺寸小于500 nm、呈球形且表面光滑的脂质包衣白藜芦醇纳米晶体。它们的溶解速度比粗白藜芦醇粉末更快。研磨过程并未损害白藜芦醇的抗氧化性能。在给大鼠口服后评估了脂质包衣白藜芦醇纳米晶体的体内药代动力学，并使用市售的植物药配方进行比较。观察到白藜芦醇曲线下面积增加，且脂质包衣纳米晶体制剂导致该化合物的口服生物利用度提高。
