title: Paclitaxel-loaded poly(n-butylcyanoacrylate) nanoparticle delivery system to overcome multidrug resistance in ovarian cancer.
abstract: OBJECTIVE
  The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism.
  
  
  METHODS
  We prepared paclitaxel-loaded PBCA nanoparticles by interfacial polymerization method. The physicochemistry of the nanoparticles was characterized. The cytotoxicity of paclitaxel-loaded PBCA nanoparticles was measured by MTT assay. Calcein-AM assay was used to analyze the P-glycoprotein (P-gp) function, and the expression of MDR-1 mRNA in A2780/T cells treated with drug-loaded nanoparticles was defined by QRT-PCR.
  
  
  RESULTS
  The nanoparticles were approximately spherical in shape with an average diameter of 224.5 ± 5.7 nm. The encapsulation efficiency was 99.23%. The in vitro drug release profile exhibited a biphasic pattern. The drug formulated in PBCA nanoparticles showed a greater cytotoxicity than paclitaxel against A2780/T cells. Paclitaxel-loaded PBCA as well as blank PBCA nanoparticles decreased P-gp function in a dose-dependent manner, suggesting the efficacy of the drug-loaded nanoparticle system on overcoming MDR. There was no significant effect on inhibition to the expression of MDR1 mRNA.
  
  
  CONCLUSIONS
  Paclitaxel-loaded PBCA nanoparticles can enhance cytotoxicity and overcome MDR through a mechanism of the inhibition of P-gp function caused by the nanoparticles system.
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, 510515, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Ren
authors.forename: Ruda
authors.initials: R
authors.lastname: Chen
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Yabin
authors.initials: Y
authors.lastname: Sun
authors.forename: Yaodong
authors.initials: Y
authors.lastname: Jiang
authors.forename: Guofeng
authors.initials: G
authors.lastname: Li
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000502:physiology; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000494:pharmacology; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D004659:Enbucrilate / Q000737:chemistry*; D005260:Female; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D010051:Ovarian Neoplasms / Q000378:metabolism / Q000473:pathology; D017239:Paclitaxel / Q000008:administration & dosage* / Q000494:pharmacology; D010316:Particle Size; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012995:Solubility; D013499:Surface Properties
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D004659:Enbucrilate; D017239:Paclitaxel