Background: Curcumin is a natural hydrophobic product showing anticancer activity. Many studies show
its potential use in the field of cancer treatment due to its safety and efficiency. However, its application is limited due
to its low water-solubility and poor selective delivery to cancer.
Objective: A Y-shaped folic acid-modified poly (ethylene glycol)-b-poly (ε-caprolactone)2 copolymer was prepared to
improve curcumin solubility and realize its selective delivery to cancer.
Method and Results: The copolymer was synthesized through selective acylation reaction of folic acid with α-
monoamino poly(ethylene glycol)-b-poly(ε-caprolactone)2. Curcumin was encapsulated into the copolymeric micelles
with 93.71% of encapsulation efficiency and 11.94 % of loading capacity. The results from confocal microscopy and
cellular uptake tests showed that folic acid-modified copolymeric micelles could improve cellular uptake of curcumin
in Hela and HepG2 cells compared with folic acid-unmodified micelles. In vitro cytotoxicity assay showed that folic
acid-modified micelles improved anticancer activity against Hela and HepG2 cells in comparison to folic acidunmodified
micelles. Meanwhile, both drug-loaded micelles demonstrated higher activity against Hela cell lines than
Conclusion: The research results suggested that the folic acid-modified Y-shaped copolymeric micelles should be used
to enhance hydrophobic anticancer drugs’ solubility and their specific delivery to folic acid receptors-overexpressed