title: Galactosylated chitosan-polycaprolactone nanoparticles for hepatocyte-targeted delivery of curcumin.
abstract: Galactosylated chitosan-polycaprolactone (Gal-CH-PCL) copolymers with a galactosylation degree of around 10% and varied PCL percentages less than 40 wt% were synthesized and used to produce nanoparticles for delivering curcumin. Some nanoparticles with encapsulation efficiency of 70% or higher and sizes changing from 100 to 250 nm were able to deliver curcumin in a controlled manner. PCL content in Gal-CH-PCLs was found to be a key factor for governing the release behavior of nanoparticles. Hepatocyte-targeted characteristic of nanoparticles was confirmed using human hepatocellular carcinoma (HepG2) cells. In comparison to free curcumin, curcumin-loaded Gal-CH-PCL nanoparticles well retained its anticancer activity. At an equivalent curcumin-dose of around 20 μg/mL that was found to be relatively safe to human normal liver cells, the results obtained from flow-cytometry revealed that some optimized Gal-CH-PCL nanoparticles showed more than 6-fold increasing abilities to induce the apoptosis and necrosis of HepG2 cells during 72 h treatment compared to free curcumin.
authors.affiliation: The Affiliated Stomatology Hospital, Guangxi Medical University, Nanning 530021, PR China.
authors.forename: Nuo
authors.initials: N
authors.lastname: Zhou
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Zan
authors.forename: Zheng
authors.initials: Z
authors.lastname: Wang
authors.forename: Hua
authors.initials: H
authors.lastname: Wu
authors.forename: Dengke
authors.initials: D
authors.lastname: Yin
authors.forename: Chunyan
authors.initials: C
authors.lastname: Liao
authors.forename: Ying
authors.initials: Y
authors.lastname: Wan
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry*; D003474:Curcumin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D005690:Galactose / Q000737:chemistry*; D006031:Glycosylation; D006367:HeLa Cells; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007700:Kinetics; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D011091:Polyesters; C016240:polycaprolactone; D048271:Chitosan; D003474:Curcumin; D005690:Galactose