Department of Microbiology and Pathology, Faculty of Veterinary Medicine, University Putra Malaysia, Serdang, Selangor, Malaysia.
Int J Nanomedicine. 2013;8:2769-81. doi: 10.2147/IJN.S45313. Epub 2013 Aug 2.
Zerumbone, a natural dietary lipophilic compound with low water solubility (1.296 mg/L at 25°C) was used in this investigation. The zerumbone was loaded into nanostructured lipid carriers using a hot, high-pressure homogenization technique. The physicochemical properties of the zerumbone-loaded nanostructured lipid carriers (ZER-NLC) were determined. The ZER-NLC particles had an average size of 52.68 ± 0.1 nm and a polydispersity index of 0.29 ± 0.004 μm. Transmission electron microscopy showed that the particles were spherical in shape. The zeta potential of the ZER-NLC was -25.03 ± 1.24 mV, entrapment efficiency was 99.03%, and drug loading was 7.92%. In vitro drug release of zerumbone from ZER-NLC was 46.7%, and for a pure zerumbone dispersion was 90.5% over 48 hours, following a zero equation. Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay in human T-cell acute lymphoblastic leukemia (Jurkat) cells, the half maximal inhibitory concentration (IC50) of ZER-NLC was 5.64 ± 0.38 μg/mL, and for free zerumbone was 5.39 ± 0.43 μg/mL after 72 hours of treatment. This study strongly suggests that ZER-NLC have potential as a sustained-release drug carrier system for the treatment of leukemia.
姜烯酮是一种天然的亲脂性膳食化合物，水溶性低（25°C 时为 1.296mg/L），本研究中使用了这种化合物。采用热高压匀化技术，将姜烯酮载入纳米结构脂质载体。对载姜烯酮纳米结构脂质载体（ZER-NLC）的理化性质进行了测定。ZER-NLC 颗粒的平均粒径为 52.68±0.1nm，多分散指数为 0.29±0.004μm。透射电子显微镜显示，颗粒呈球形。ZER-NLC 的 Zeta 电位为-25.03±1.24mV，包封率为 99.03%，载药量为 7.92%。在体外，ZER-NLC 中姜烯酮的释放 48 小时后达到 46.7%，而纯姜烯酮分散体达到 90.5%，符合零级方程。采用 MTT（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐）法，在人 T 细胞急性淋巴细胞白血病（Jurkat）细胞中，ZER-NLC 的半最大抑制浓度（IC50）为 5.64±0.38μg/mL，72 小时后游离姜烯酮的 IC50 为 5.39±0.43μg/mL。本研究强烈表明，ZER-NLC 有望成为治疗白血病的一种新型缓释药物载体系统。
