Si-Yong Qin,a,b Meng-Yun Peng, a Lei Rong, a Hui-Zhen Jia, a Si Chen, a Si-Xue Cheng, a Jun Feng, a Xian-Zheng Zhang*a
aKey Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, China.
bSchool of Chemistry and Materials Science, South-Central University for Nationalities, Wuhan 430074, China
Nanoscale, Volume 7, 5 August 2015, Pages 14786–14793.
A programmed pre-targeting system for tumor cell imaging and targeting therapy was established based on the“biotin–avidin”interaction. In this programmed functional system, transferrin-biotin can be actively captured by tumor cells with the overexpression of transferrin receptors, thus achieving the pre-targeting modality. Depending upon avidin–biotin recognition, the attachment of multivalent FITC–avidin to biotinylated tumor cells not only offered the rapidfluorescence labelling, but also endowed the pre-targeted cells with targeting sites for the specifically designed biotinylated peptide nano-drug. Owing to the successful pre-targeting, tumorous HepG2 and HeLa cells were effectively distinguished from the normal 3T3 cells via fluorescence imaging. In addition, the self-assembled peptide nano-drug resulted in enhanced cell apoptosis in the observed HepG2 cells. The tumor cell specific pre-targeting strategy is applicable for a variety of different imaging and therapeutic agents for tumor treatments.