Folate receptor (FR) is well known for its overexpression on surface of various cancer cell lines, which is identical to normal tissue. Folic-based targeting drug delivery systems, therefore, are one of the most effective targeting carriers that effectively bind to FR up-regulated cancer cells. Curcumin was used both for labeling and chemotherapy. The materials were characterized and structurally confirmed by FT-IR spectra, fluorescent images and FE-SEM images. Bioassays were conducted on HeLa and HT29 cancer cell lines after 4 and 12 hours. Results show that folic acid significantly enhanced both targeting efficiency and internalization of curcumin to FR-expressing cancer cells