Wu Shichao, Yang Xiangrui, Li Yang, Wu Hongjie, Huang Yu, Xie Liya, Zhang Ying, Hou Zhenqing, Liu Xiangyang
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China.
Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, 361005, China.
Nanoscale Res Lett. 2016 Dec;11(1):294. doi: 10.1186/s11671-016-1491-9. Epub 2016 Jun 14.
The high-aspect-ratio nanoparticles were proved to be internalized much more rapidly and efficiently by cancer cells than the nanoparticles with an equal aspect ratio. Herein, a kind of high-aspect ratio, pointed-end nanoneedles (NDs) with a high drug loading (15.04 %) and the prolonged drug release profile were fabricated with an anti-tumor drug-10-hydroxycamptothecin (HCPT)-via an ultrasound-assisted emulsion crystallization technique. It is surprising to see that the cellular internalization of NDs with an average length of 5 μm and an aspect ratio of about 12:1 was even much faster and higher than that of nanorods with the same size and the nanospheres with a much smaller size of 150 nm. The results further validated that cellular internalization of the nanoparticles exhibited a strong shape-dependent effect, and cellular uptake may favor the particles with sharp ends as well as a high-aspect ratio instead of particle size. The NDs with enhanced cytotoxicity would lead to a promising sustained local drug delivery system for highly efficient anticancer therapy. More importantly, the fabrication of NDs opens a door to design new formulations of nanoneedle drug delivery systems for highly efficient cancer.
实验证明，与具有相同长径比的纳米颗粒相比，高长径比的纳米颗粒能更快、更有效地被癌细胞内化。在此，通过超声辅助乳液结晶技术，制备了一种高长径比、尖端尖锐的纳米针（NDs），其载药量高（15.04%）且药物释放曲线延长，负载的抗肿瘤药物为10-羟基喜树碱（HCPT）。令人惊讶的是，平均长度为5μm、长径比约为12:1的NDs的细胞内化速度甚至比相同尺寸的纳米棒以及尺寸小得多的150nm纳米球还要快、还要高。结果进一步证实，纳米颗粒的细胞内化表现出强烈的形状依赖性效应，细胞摄取可能更倾向于具有尖锐末端和高长径比的颗粒，而非颗粒大小。具有增强细胞毒性的NDs将为高效抗癌治疗带来一种有前景的持续局部给药系统。更重要的是，NDs的制备为设计用于高效癌症治疗的新型纳米针药物递送系统开辟了道路。
