Self-Assembly of Folate onto Polyethyleneimine-Coated CdS/ZnS Quantum Dots for Targeted Turn-On Fluorescence Imaging of Folate Receptor Overexpressed Cancer Cells

Folate receptor (FR) can be overexpressed by a number of epithelial-derived tumors, but minimally expressed in normal tissues. As folic acid (FA) is a high-affinity ligand to FR, and not produced endogenously, development of FA-conjugated probes for targeted imaging FR overexpressed cancer cells is of significance for assessing cancer therapeutics and for better understanding the expression profile of FR in cancer. Here we report a novel turn-on fluorescence probe for imaging FR overexpressed cancer cells. The probe was easily fabricated via electrostatic self-assembly of FA and polyethyleneimine-coated CdS/ZnS quantum dots (PEI-CdS/ZnS QDs). The primary fluorescence of PEI-CdS/ZnS QDs turned off first upon the electrostatic adsorption of FA onto PEI-CdS/ZnS QDs based on electron transfer to produce negligible fluorescence background. The presence of FR expressed on the surface of cancer cells then made FA desorb from PEI-CdS/ZnS QDs due to specific and high affinity of FA to FR. As a result, the primary fluorescence of PEI-CdS/ZnS QDs adhering to the cells turned on due to the inhibition of electron transfer. The most important merits of the developed probe are its simplicity and the effective avoidance of the false positive results due to the simple electrostatic self-assembly of FA onto the surface of PEI-CdS/ZnS QDs and the involved fluorescence "off-on" mechanism. The probe was demonstrated to be sensitive and selective for targeted imaging of FR overexpressed cancer cells in turn-on mode.