title: An efficient injectable formulation with block copolymer micelles for hydrophobic antitumor candidate-pyridazinone derivatives.
abstract: OBJECTIVE
  To make delivery improvements via delivery systems for 6-(4-morpholino-3-(trifluoromethyl)phenyl)pyridazin-3(2H)-one (DZO) - a model compound of hydrophobic antitumor candidate pyridazinone derivatives.
  
  
  METHODS
  Methoxy poly(ethylene glycol)-poly(D,L-lactide) (MPEG-PDLLA) micelle was employed as a vector, and DZO was encapsulated in. The DZO-loaded micelles were characterized in detail and its cytotoxicity, maximum tolerated dose (MTD) and pharmacokinetic experiments were done. In vivo anticancer activity was studied through a subcutaneous 4T1 tumor model.
  
  
  RESULTS
  Compared with free DZO, the DZO-loaded micelles possessed a sustained release property, an improved MTD, better pharmacokinetic parameters and an enhanced antitumor activity for subcutaneous 4T1 model in vivo.
  
  
  CONCLUSIONS
  An effective injectable delivery system for DZO was developed successfully.
authors.affiliation: State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.|Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu, China.
authors.forename: XiuXiu
authors.initials: X
authors.lastname: Jin
authors.affiliation: State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.
authors.forename: YaLi
authors.initials: Y
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.
authors.forename: LiWei
authors.initials: L
authors.lastname: Tan
authors.affiliation: Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: He
authors.affiliation: State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.
authors.forename: JinRong
authors.initials: J
authors.lastname: Peng
authors.affiliation: Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu, China.
authors.forename: Li
authors.initials: L
authors.lastname: Hai
authors.affiliation: Key Laboratory of Drug Targeting of Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu, China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.
authors.forename: ZhiYong
authors.initials: Z
authors.lastname: Qian
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D008823:Micelles; D011108:Polymers / Q000737:chemistry*; D011724:Pyridazines / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use; D051381:Rats; D023041:Xenograft Model Antitumor Assays
chemical_list: D008823:Micelles; D011108:Polymers; D011724:Pyridazines; D004317:Doxorubicin
keywords: MPEG-PDLLA micelle; antitumor; delivery system; hydrophobic; pyridazinone derivative