To engineer multifunctional nanomedicines for simultaneous imaging and therapy of cancer cells, we have prepared Gambogenic acid (GNA) loaded folic acid (FA) armed MNPs (FA-GNA-MNPs) to target the folate receptor (FR) positive cancer cells. The FA-GNA-MNPs have been prepared by a facile method, which have been further characterized by SEM, TEM, IR and UV-vis spectra. And the cytotoxicity of FA-GNA-MNPs to HeLa and A549 cells was assessed using the MTT assay. The FA-GNA-MNPs (with loading efficiency of 4.35%) showed sustained liberation of GNA molecules (with 73.46% release in 96 h). The mean particle diameter (MD) of FA-GNA-MNPs and the polydispersity index (PDI) are 254.3 nm and 0.139, respectively. The cytotoxicity of free GNA and FA-GNA-MNPs toward HeLa cells showed that FA-GNA-MNPs was more cytotoxic than GNA. Based on these findings, it suggests that FA-GNA-MNPs would be as a novel multifunctional nanomedicine/theranostic for concurrent targeting, imaging and therapy of the FR-positive cancer cells.