Efficacy of NGR peptide-modified PEGylated quantum dots for crossing the blood-brain barrier and targeted fluorescence imaging of glioma and tumor vasculature.
Delivery of imaging agents to brain glioma is challenging because the blood-brain barrier (BBB) functions as a physiological checkpoint guarding the central nervous system from circulating large molecules. Moreover, the ability of existing probes to target glioma has been insufficient and needs to be improved. In present study, PEG-based long circulation, CdSe/ZnS quantum dots (QDs)-based nanoscale and fluorescence, asparagines-glycine-arginine peptides (NGR)-based specific CD13 recognition were integrated to design and synthesize a novel nanoprobe by conjugating biotinylated NGR peptides to avidin-PEG-coated QDs. Our data showed that the NGR-PEG-QDs were nanoscale with less than 100 nm and were stable in various pH (4.0~8.0). These nanomaterials with non-toxic concentrations could cross the BBB and target CD13-overexpressing glioma and tumor vasculature in vitro and in vivo, contributing to fluorescence imaging of this brain malignancy. These achievements allowed groundbreaking technological advances in targeted fluorescence imaging for the diagnosis and surgical removal of glioma, facilitating potential transformation toward clinical nanomedicine.
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Ning
N
Huang
Department of Orthopaedics, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Si
S
Cheng
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China; Chongqing Key Laboratory of Ultrasound Molecular Imaging, Institute of Ultrasound Imaging of Chongqing Medical University, Chongqing, China.
Xiang
X
Zhang
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China; Institute of Life Sciences, Chongqing Medical University, Chongqing, China.
Qi
Q
Tian
College of Chemistry and Chemical Engineering, Southwest University, Chongqing, China.
Jiangli
J
Pi
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Jun
J
Tang
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Qing
Q
Huang
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Feng
F
Wang
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Jin
J
Chen
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Zongyi
Z
Xie
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Zhongye
Z
Xu
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Weifu
W
Chen
College of Chemistry and Chemical Engineering, Southwest University, Chongqing, China.
Huzhi
H
Zheng
Department of Neurosurgery, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, China. Electronic address: chengyuan023@aliyun.com.
Yuan
Y
Cheng
D000818:Animals; D001812:Blood-Brain Barrier; D001932:Brain Neoplasms / Q000098:blood supply / Q000000981:diagnostic imaging*; D005453:Fluorescence; D005910:Glioma / Q000098:blood supply / Q000000981:diagnostic imaging*; D008297:Male; D009374:Neoplasms, Experimental / Q000098:blood supply / Q000000981:diagnostic imaging; D009842:Oligopeptides / Q000737:chemistry*; D061848:Optical Imaging; D045663:Quantum Dots / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley
D009842:Oligopeptides; C000615951:asparagine-glycine-arginine
Blood–brain barrier; Brain glioma; CD13; NGR; Quantum dot