In this study, glycyrrhetinic acid (GA) was conjugated with mono amino poly (ethylene glycol)-b-poly (epsilon-caprolactone) (H2N-PEG-PCL) with sucdnate linker to obtain the GA-modified PEG-PCL (GA-PEG-Pa). By way of thin film hydration method, curcumin was encapsulated into GA-PEG-PCL copolymer to form stable micelles with 93.76% of encapsulation efficiency and 11.93% of drug loading capacity. The micelles enhanced curcumin's water-solubility to 1.87 mg/ml, being 1.70 x 10(5) times higher than free curcumin. X-ray diffraction and FT-IR analysis confirmed the encapsulation of CUR into copolymeic micelles with an amorphous state. Hemolysis datum of blank micelles showed its biocompatibility. Compared with GA-unconjugated micelles, curcumin-loaded GA-PEG-PCL micelles showed slower in vitro release of drug, but they displayed better in vitro cytotoxicity against HepG2 at about 40 mu M because of its selective accumulation in HepG2 cells induced by GA. The results showed that GA-PEG-PCL copolymer could be a promising drug carrier for liver targeted drug delivery. (C) 2016 Elsevier B.V. All rights reserved.