title: A novel preparation method of paclitaxcel-loaded folate-modified chitosan microparticles and in vitro evaluation.
abstract: A new chitosan microparticles loading paclitaxel (PTX) for application as an oral delivery system were developed using a novel double emulsion crosslinking method. To improve the targeted effect, folic acid (FA) was introduced onto the surface of microparticles using chemical method. The method was based on Schiff reaction between amino group of chitosan and carboxyl group of FA, and folate-chitosan (FA-CS) conjugate was characterized using infrared spectrum analysis (FT-IR), and the microparticles were named as FA-CS-PTX/MPs. FA-CS-PTX/MPs had larger size of average diameter 223.6 nm, while PTX-loaded chitosan microparticles (CS-PTX/MPs) had 179.1 nm average diameter. The zeta potential of CS-PTX/MPs and FA-CS-PTX/MPs was 22.3 and 33.1 mV, respectively. SEM and TEM showed both the two microparticles had well-defined spherical structure. The in vitro drug release was studied under different pH conditions, and a two-phase kinetics model was found to be the most adequate kinetic model. Furthermore, the cytotoxicity activities of drug-carriers against L929 cells and the cellular uptake of PTX-loaded microparticles against HepG2 cells were investigated. Results demonstrated that FA-CS-PTX/MPs might be a promising drug carrier for promoting PTX cellular uptake and could be used as a potential tumor-targeted drug vector.
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.|b Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals , Nanjing , P.R.China.
authors.forename: Fang
authors.initials: F
authors.lastname: Wang
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.
authors.forename: Siqian
authors.initials: S
authors.lastname: Yang
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.|b Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals , Nanjing , P.R.China.
authors.forename: Dawei
authors.initials: D
authors.lastname: Hua
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.
authors.forename: Jian
authors.initials: J
authors.lastname: Yuan
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.|b Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals , Nanjing , P.R.China.
authors.forename: Chaobo
authors.initials: C
authors.lastname: Huang
authors.affiliation: a College of Chemical Engineering, Nanjing Forestry University , Nanjing , P.R. China.|b Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals , Nanjing , P.R.China.
authors.forename: Qinwei
authors.initials: Q
authors.lastname: Gao
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D048271:Chitosan / Q000737:chemistry; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D065546:Drug Liberation; D005347:Fibroblasts / Q000187:drug effects / Q000502:physiology; D005492:Folic Acid / Q000737:chemistry; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy / Q000503:physiopathology; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D048271:Chitosan; D005492:Folic Acid; D017239:Paclitaxel
keywords: Paclitaxel; chitosan; folic acid; microparticle; tumor targeting