Original articles
Han Xiao, Rui Zhang, Xiaobo Fan, Xinglu Jiang, Mingyuan Zou, Xuejiao Yan, Haiping Hao, Guoqiu Wu. Super-sensitive bifunctional nanoprobe: Self-assembly of peptide-driven nanoparticles demonstrating tumor fluorescence imaging and therapy[J]. Acta Pharmaceutica Sinica B, 2022, 12(3): 1473-1486

Super-sensitive bifunctional nanoprobe: Self-assembly of peptide-driven nanoparticles demonstrating tumor fluorescence imaging and therapy
Han Xiaoa,d, Rui Zhanga, Xiaobo Fana, Xinglu Jianga, Mingyuan Zoua, Xuejiao Yanf, Haiping Haoe, Guoqiu Wub,c
a. Medical School, Southeast University, Nanjing 210009, China;
b. Center of Clinical Laboratory Medicine, Zhongda Hospital, Southeast University, Nanjing 210009, China;
c. Jiangsu Provincial Key Laboratory of Critical Care Medicine, Southeast University, Nanjing 210009, China;
d. Department of Clinical Laboratory, the Fifth Affiliated Hospital of Sun Yat-sen University, Zhuhai 519000, China;
e. State Key Laboratory of Natural Medicines, Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 21009, China;
f. Department of Cardiology, the Affiliated Changzhou No. 2 People's Hospital of Nanjing Medical University, Changzhou 213000, China
The development of nanomedicine has recently achieved several breakthroughs in the field of cancer treatment; however, biocompatibility and targeted penetration of these nanomaterials remain as limitations, which lead to serious side effects and significantly narrow the scope of their application. The self-assembly of intermediate filaments with arginine-glycine-aspartate (RGD) peptide (RGD-IFP) was triggered by the hydrophobic cationic molecule 7-amino actinomycin D (7-AAD) to synthesize a bifunctional nanoparticle that could serve as a fluorescent imaging probe to visualize tumor treatment. The designed RGD-IFP peptide possessed the ability to encapsulate 7-AAD molecules through the formation of hydrogen bonds and hydrophobic interactions by a one-step method. This fluorescent nanoprobe with RGD peptide could be targeted for delivery into tumor cells and released in acidic environments such as endosomes/lysosomes, ultimately inducing cytotoxicity by arresting tumor cell cycling with inserted DNA. It is noteworthy that the RGD-IFP/7-AAD nanoprobe tail-vein injection approach demonstrated not only high tumor-targeted imaging potential, but also potent antitumor therapeutic effects in vivo. The proposed strategy may be used in peptide-driven bifunctional nanoparticles for precise imaging and cancer therapy.
Key words:    Nanoprobe    7-Amino actinomycin D    Intermediate filament protein    Tumor image    Antitumor therapy    Integrin αvβ3   
Received: 2021-05-13     Revised: 2021-06-22
DOI: 10.1016/j.apsb.2021.07.020
Funds: This work was supported by the National Natural Science Foundation of China (No. 81603016, 81773624, 81900453), the Natural Science Foundation of Jiangsu Province (No. BK20160706, BE2017746, China), the National Science and Technology Major Project (2018ZX09301026-005, 2020ZX09201015, China).
Corresponding author: Haiping Hao,E-mai:hhp_770505@hotmail.com;Guoqiu Wu,E-mai:101008404@seu.edu.cn     Email:hhp_770505@hotmail.com;101008404@seu.edu.cn
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Han Xiao
Rui Zhang
Xiaobo Fan
Xinglu Jiang
Mingyuan Zou
Xuejiao Yan
Haiping Hao
Guoqiu Wu

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