The g-cyclodextrin-folate (γ-CD/FA) inclusion-coated CdSe/ZnS quantum dots (QDs) with folate- receptor (FR) targeted were synthesized by simple and convenient sonochemical method.  The products were studied using fourier transform infrared (FTIR), proton nuclear magnetic resonance (¹H NMR), utraviolet-visible spectrometry (UV-vis), fluorescence spectrum and transmission electron micrographs (TEM).  The results showed that the γ-CD/FA-coated CdSe/ZnS QDs not only have good monodispersity and smaller size, but also have good optical performance, such as higher quantum yield (QY) and a long fluorescence lifetime.  The cytotoxicity experiments showed that the γ-CD/FA-coated CdSe/ZnS QDs have lower cytotoxicity and could more effectively enter cancer cells with FR over-expression.  The QDs with 4−5 nm in diameter were relatively easy to enter the cell and to be removed through kidneys, so it is more suitable for biomedical applications for bioprobes and bioimaging.