Department of Materials Science and Engineering, University of Washington, Seattle, Washington 98195, United States.
Department of Chemistry of The College of Staten Island and The Graduate Center, The City University of New York, Staten Island, New York 10314, United States.
Nanoscale. 2017 Jan 26;9(4):1434-1442. doi: 10.1039/c6nr07894j.
Loading and controlled release of sufficient hydrophobic drugs to tumor cells has been the bottleneck in chemotherapy for decades. Herein we report the development of a fluorescent and mesoporous carbon nanoshell (FMP-CNS) that exhibits a loading capacity for the hydrophobic drug paclitaxel (PTX) as high as ∼80 wt% and releases the drug in a controllable fashion under NIR irradiation (825 nm) at an intensity of 1.5 W cm. The high drug loading is primarily attributed to its mesoporous structure and to the supramolecular π-stacking between FMP-CNSs and PTX molecules. The FMP-CNS also exhibits wavelength-tunable and upconverted fluorescence properties and thus can serve as an optical marker for confocal, two-photon, and near infrared (NIR) fluorescence imaging. Furthermore, our in vitro results indicate that FMP-CNSs demonstrate high therapeutic efficacy through the synergistic effect of combined chemo-photothermal treatment. In vivo studies demonstrate marked suppression of tumor growth in mice bearing rat C6 glioblastoma after administration with a single intratumoral injection of PTX-loaded FMP-CNS.
数十年来,向肿瘤细胞有效加载并控制释放足够量的疏水性药物一直是化疗的瓶颈。在此,我们报告了一种荧光介孔碳纳米壳(FMP-CNS)的研制,其对疏水性药物紫杉醇(PTX)的载药能力高达约 80wt%,并在近红外辐射(825nm)下以 1.5Wcm 的强度实现药物的可控释放。高载药量主要归因于其介孔结构以及 FMP-CNS 与 PTX 分子之间的超分子π堆积。FMP-CNS 还表现出波长可调谐的上转换荧光特性,因此可用作共聚焦、双光子和近红外(NIR)荧光成像的光学标记物。此外,我们的体外研究结果表明,FMP-CNS 通过化学-光热联合治疗的协同作用表现出很高的治疗效果。体内研究表明,荷大鼠 C6 神经胶质瘤瘤小鼠经单次瘤内注射载 PTX 的 FMP-CNS 给药后,肿瘤生长得到显著抑制。