Curcumin, as a naturally occurring polyphenol, has been extensively used as anticancer and antioxidant agent due to its ability to protect cells from oxidative damage. However, its poor solubility and low bioavailability have limited its application. To increase the solubility and effectiveness of curcumin, a new multi-drug delivery system is developed based on curcumin-loaded cyclodextrin-conjugated gallic acid. For this purpose, beta-cyclodextrin was grafted by gallic acid, and then, a 2:1 inclusion complex of cyclodextrin and curcumin was prepared. The mean particle size of the curcumin-loaded beta-CD-g-GA was about 100 nm by DLS. All observations using FT-IR, NMR, UV-Vis and FE-SEM confirmed successful preparation of the CUR@beta-CD-graft-gallic acid. In addition, antioxidant activity and release behavior of the curcumin-loaded beta-CD-graft-GA was investigated. The IC50 value for CUR@beta-CD-g-GA was estimated (0.4909 mu g/mL) based on their inhibition percent-concentration curves using DPPH assay. Also, the total released amount of curcumin within 48 h in pH 7.4 and 5.4 was 41% and 91%, respectively. Because the designed multi-drug delivery system is convenient to prepare, possesses appropriate antioxidant activity and pH-sensitive release behavior and most importantly composed of fully green and safe materials, it may represent an attractive new potent multi-drug delivery system.