title: PEG-coated irinotecan cationic liposomes improve the therapeutic efficacy of breast cancer in animals.
abstract: BACKGROUND
  Breast cancer is the most frequently diagnosed cancer and the leading cause of cancer death among females owing.
  
  
  OBJECTIVE
  This study aimed to construct a kind of PEG-coated irinotecan cationic liposomes for investigating its efficacy and mechanism of action in the treatment of breast cancer in preclinical models.
  
  
  METHODS
  Evaluations were performed on the MDA-MB231 breast cancer cells, the xenografted MDA-MB231 cancer cells in Female nude mice and Sprague-Dawley (SD) rat. The liposomes were characterized through assays of cytotoxicity, intracellular uptake, nuclei morphology, antitumor activities, pharmacokinetics and tissue distribution.
  
  
  RESULTS
  The zeta potential of PEG-coated irinotecan cationic liposomes was approximately 23 mV. The PEG-coated irinotecan cationic liposomes were approximately 66nm in diameter, significantly increased the intracellular uptake of irinotecan, and showed strong inhibitory effect on MDA-MB231 breast cancer cells. A significant antitumor efficacy in the xenografted MDA-MB231 breast cancer cells in nude mice was evidenced by intravenous administration of PEG-coated irinotecan cationic liposomes. PEG-coated irinotecan cationic liposomes also improved the irinotecan blood circulation time and showed an enhanced drug concentration in tumor.
  
  
  CONCLUSIONS
  PEG-coated irinotecan cationic liposomes had significant inhibitory effect against breast cancer in vitro and in vivo, hence providing a new strategy for treating breast cancer.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Hebei Medical University, Research Center of Chinese Medicine Injection in Hebei Province, Shijiazhuang, China. cao_dy@126.com.
authors.forename: L
authors.initials: L
authors.lastname: Zhang
authors.forename: D-Y
authors.initials: DY
authors.lastname: Cao
authors.forename: J
authors.initials: J
authors.lastname: Wang
authors.forename: B
authors.initials: B
authors.lastname: Xiang
authors.forename: J-N
authors.initials: JN
authors.lastname: Dun
authors.forename: Y
authors.initials: Y
authors.lastname: Fang
authors.forename: G-Q
authors.initials: GQ
authors.lastname: Xue
mesh_terms: D000818:Animals; D001853:Bone Marrow / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002412:Cations; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D007275:Injections, Intravenous; D000077146:Irinotecan; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013499:Surface Properties; D014018:Tissue Distribution; D059004:Topoisomerase I Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D023041:Xenograft Model Antitumor Assays
chemical_list: D002412:Cations; D008055:Lipids; D008081:Liposomes; D059004:Topoisomerase I Inhibitors; D011092:Polyethylene Glycols; D000077146:Irinotecan; D002166:Camptothecin