State Key Laboratory of Food Science and Technology, Jiangnan University, Wuxi, Jiangsu 214122, P. R. China.
Soft Matter. 2021 Mar 28;17(12):3306-3313. doi: 10.1039/d0sm01655a. Epub 2021 Feb 24.
Inverse bicontinuous cubic phase nanoparticles (cubosomes) have attracted significant attention in recent years, owing to their potential use as delivery vehicles for chemically fragile or poorly soluble drugs and nutraceuticals. Herein we have investigated the use of lipid nanoparticles as a delivery vehicle for curcumin, a compound with demonstrated anti-cancer properties. Curcumin is encapsulated within cubosomes comprised of several different lipid formulations, as well as phospholipid-based liposomes. The entrapment efficiency of curcumin within cubosomes was observed to vary depending on both the nanoparticle architecture and the curcumin concentration. Fluorescence spectroscopy analysis revealed that penetration of curcumin into the hydrophobic region of the bilayer was dependent on lipid composition. Curcumin was typically associated with the polar headgroup region at low concentrations, but transferred to the lipid bilayer region at higher concentrations, particularly in phytantriol cubosomes. Each nanoparticle formulation was characterized using small angle X-ray scattering and dynamic light scattering to assess the structural stability subsequent to curcumin encapsulation. The structure of the cubosomes was generally robust to the addition of curcumin, while the liposomes displayed a large increase in particle size and PDI at higher curcumin concentrations. Finally, the cytotoxicity of each formulation was assessed against murine fibroblast (NIH3T3) and murine melanoma (B16F10) cell lines in order to investigate improvements in curcumin bioavailability following encapsulation in cubosomes, as well as assess potential anti-cancer applications. Increased cytotoxicity of the cubosome-loaded curcumin against the murine melanoma cell-line demonstrates the potential of these nanoparticles as delivery vehicles for curcumin and other poorly water-soluble drugs.
近年来,反向双连续立方相纳米颗粒(立方脂质体)因其可能作为化学脆弱或水溶性差的药物和营养保健品的递送载体而受到广泛关注。本文研究了脂质纳米颗粒作为姜黄素递送载体的用途,姜黄素已被证明具有抗癌特性。姜黄素被包封在由几种不同脂质配方以及基于磷脂的脂质体组成的立方脂质体中。观察到姜黄素在立方脂质体中的包封效率取决于纳米颗粒结构和姜黄素浓度。荧光光谱分析表明,姜黄素渗透到双层的疏水区取决于脂质组成。在低浓度时,姜黄素通常与极性头部基团区域相关,但在高浓度时,特别是在植烷三醇立方脂质体中,转移到脂质双层区域。使用小角 X 射线散射和动态光散射对每种纳米颗粒制剂进行表征,以评估姜黄素包封后结构的稳定性。立方脂质体的结构通常对添加姜黄素具有很强的稳定性,而脂质体在更高的姜黄素浓度下显示出粒径和 PDI 的大幅增加。最后,评估了每种制剂对小鼠成纤维细胞(NIH3T3)和小鼠黑色素瘤(B16F10)细胞系的细胞毒性,以研究姜黄素在立方脂质体包封后生物利用度的提高,并评估其作为姜黄素和其他水溶性差的药物的潜在抗癌应用。负载姜黄素的立方脂质体对小鼠黑色素瘤细胞系的细胞毒性增加证明了这些纳米颗粒作为姜黄素和其他水溶性差的药物的递送载体的潜力。