title: Y-shaped Folic Acid-Conjugated PEG-PCL Copolymeric Micelles for Delivery of Curcumin.
abstract: 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.
  
  
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
authors.forename: Runliang
authors.initials: R
authors.lastname: Feng
authors.affiliation: School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
authors.forename: Wenxia
authors.initials: W
authors.lastname: Zhu
authors.affiliation: National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, No.15 Datun Road, Chaoyang District, Beijing 100101, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Chu
authors.affiliation: School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, No.l6866 East Road of Jingshi, Jinan 250200, Shandong Province, China.
authors.forename: Fangfang
authors.initials: F
authors.lastname: Teng
authors.affiliation: School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Meng
authors.affiliation: School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
authors.forename: Peizong
authors.initials: P
authors.lastname: Deng
authors.affiliation: Department of Pharmaceutical Engineering, School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
authors.forename: Zhimei
authors.initials: Z
authors.lastname: Song
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D005026:Ethylene Glycols / Q000737:chemistry*; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism; D005492:Folic Acid / Q000737:chemistry* / Q000378:metabolism; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D008823:Micelles; D015394:Molecular Structure; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship; D013499:Surface Properties
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005026:Ethylene Glycols; D058973:Folate Receptors, GPI-Anchored; D008823:Micelles; D011091:Polyesters; C476300:poly(epsilon-caprolactone)-b-poly(ethylene glycol); D005492:Folic Acid; D003474:Curcumin
keywords: Curcumin; Y-shaped; copolymer; folic acid; poly (ethylene glycol); ε-caprolactone