Runliang Feng, Wenxia Zhu, Wei Chu, Fangfang Teng, Ning Meng, Peizong Deng and Zhimei Song Pages 599 - 607 ( 9 )
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. <p></p> 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. <p></p> 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 HepG2. <p></p> 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 cancer. <p></p>
Curcumin, folic acid, poly (ethylene glycol), ε-caprolactone, Y-shaped, copolymer.
School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, No.15 Datun Road, Chaoyang District, Beijing 100101, School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, No.l6866 East Road of Jingshi, Jinan 250200, Shandong Province, School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, Department of Pharmaceutical Engineering, School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province