Preparation of HCPT-Loaded Nanoneedles with Pointed Ends for Highly Efficient Cancer Chemotherapy.
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.
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.
Shichao
S
Wu
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China.
Xiangrui
X
Yang
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China.
Yang
Y
Li
School of Pharmaceutical Sciences, Xiamen University, Xiamen, 361005, China.
Hongjie
H
Wu
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China.
Yu
Y
Huang
The First Affiliated Hospital of Xiamen University, Xiamen, 361002, China. xly885@163.com.
Liya
L
Xie
Department of Radiology, Taishan Medical University, Tai'an, China.
Ying
Y
Zhang
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China. houzhenqing@xmu.edu.cn.
Zhenqing
Z
Hou
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China. Liuxy@xmu.edu.cn.
Xiangyang
X
Liu
Cellular uptake; HCPT; High-aspect ratio; Pointed-end