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载姜黄素纳米脂质体的纳米级特征定位。

Curcumin Loaded Nanoliposomes Localization by Nanoscale Characterization.

机构信息

LIBio, Université de Lorraine, F-54000 Nancy, France.

LCPME, CNRS-Université de Lorraine, F-54600 Villers-lès-Nancy, France.

出版信息

Int J Mol Sci. 2020 Oct 1;21(19):7276. doi: 10.3390/ijms21197276.

DOI:10.3390/ijms21197276
PMID:33019782
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7584047/
Abstract

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.

摘要

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。

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