LIBio, Université de Lorraine, F-54000 Nancy, France.
LCPME, CNRS-Université de Lorraine, F-54600 Villers-lès-Nancy, France.
Int J Mol Sci. 2020 Oct 1;21(19):7276. doi: 10.3390/ijms21197276.
Curcumin is a hydrophobic drug gaining growing attention because of its high availability, its innocuity, and its anticancer, antitumoral, and antioxidative activity. However, its poor bioavailability in the human body, caused by its low aqueous solubility and fast degradation, presents a big hurdle for its oral administration. Here, we used nano-vesicles made of phospholipids to carry and protect curcumin in its membrane. Various curcumin amounts were encapsulated in the produced phospholipid system to form drug-loaded liposomes. Curcumin's concentration was evaluated using UV-visible measurements. The maximal amount of curcumin that could be added to liposomes was assessed. Nuclear magnetic resonance (NMR) analyses were used to determine curcumin's interactions and localization within the phospholipid membrane of the liposomes. X-ray scattering (SAXS) and atomic force microscopy (AFM) experiments were performed to characterize the membrane structure and organization, as well as its mechanical properties at the nanoscale. Conservation of the membrane's properties is found with the addition of curcumin in various amounts before saturation, allowing the preparation of a defined nanocarrier with desired amounts of the drug.
姜黄素是一种疏水性药物,由于其高可用性、无害性以及抗癌、抗肿瘤和抗氧化活性,越来越受到关注。然而,由于其在水中的溶解度低和快速降解,其在人体中的生物利用度很低,这对其口服给药构成了很大的障碍。在这里,我们使用由磷脂制成的纳米囊泡来携带和保护姜黄素在其膜内。将各种数量的姜黄素包裹在生产的磷脂系统中以形成载药脂质体。使用紫外-可见测量法评估姜黄素的浓度。评估了可以添加到脂质体中的最大姜黄素量。使用核磁共振(NMR)分析来确定姜黄素在脂质体的磷脂膜内的相互作用和定位。进行了 X 射线散射(SAXS)和原子力显微镜(AFM)实验,以在纳米尺度上表征膜结构和组织及其机械性能。在达到饱和之前,以各种量添加姜黄素后发现保留了膜的性质,从而可以制备具有所需药物量的定义明确的纳米载体。