title: PEGylated VRB plus quinacrine cationic liposomes for treating non-small cell lung cancer.
abstract: BACKGROUND
  Non-small cell lung cancer (NSCLC) is the most common form of lung cancer, and the treatment effects are usually unsatisfactory. Vinorelbine (VRB) is extensively used in cancer treatment, but it has some disadvantages when used alone. PEGylated liposomes have been extensively used as a delivery carrier for antitumor drugs via prolonging the circulation time in the blood.
  
  
  OBJECTIVE
  The nanostructured liposomes were designed and prepared for treating NSCLC.
  
  
  METHODS
  In the liposomes, PEG was modified on the liposomal surface, DC-Chol was used as cationic materials, and VRB plus quinacrine were encapsulated in an aqueous core of the liposomes as an antitumor drug and an apoptosis-inducing agent, respectively. Evaluations were performed on A549 cells, tubular network formations and xenografts of the A549 cells.
  
  
  RESULTS
  The PEGylated drugs-loaded cationic liposomes could significantly enhance cellular uptake and selectively accumulate in A549 cells, thus leading to show strongest antitumor efficacy to tumor cells and to tumor-bearing mice. Action mechanisms showed that the enhanced efficacy in treating NSCLC was related to activate caspase 9 and caspase 3, to activate Bax and P53, and to suppress Bcl-2 and Mcl-1.
  
  
  CONCLUSIONS
  The PEGylated VRB plus quinacrine cationic liposomes showed a potential strategy for treating NSCLC.
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine , Dalian , China and.
authors.forename: Xue-Tao
authors.initials: XT
authors.lastname: Li
authors.forename: Zhi-Yan
authors.initials: ZY
authors.lastname: Zhou
authors.forename: Ying
authors.initials: Y
authors.lastname: Jiang
authors.forename: Mei-Li
authors.initials: ML
authors.lastname: He
authors.forename: Lian-Qun
authors.initials: LQ
authors.lastname: Jia
authors.forename: Lin
authors.initials: L
authors.lastname: Zhao
authors.forename: Lan
authors.initials: L
authors.lastname: Cheng
authors.forename: Tian-Zhu
authors.initials: TZ
authors.lastname: Jia
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D051017:Apoptosis Regulatory Proteins / Q000378:metabolism; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy*; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006801:Humans; D008081:Liposomes; D008175:Lung Neoplasms / Q000188:drug therapy*; D008297:Male; D051379:Mice; D011092:Polyethylene Glycols / Q000737:chemistry*; D011796:Quinacrine / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D014747:Vinblastine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000077235:Vinorelbine; D023041:Xenograft Model Antitumor Assays
chemical_list: D051017:Apoptosis Regulatory Proteins; D008081:Liposomes; D011092:Polyethylene Glycols; D014747:Vinblastine; D011796:Quinacrine; D000077235:Vinorelbine
keywords: Liposomes; solid tumor; targeted drug delivery; tumor targeting