title: Construction of amphiphilic copolymer nanoparticles based on hyperbranched poly (amine-ester) and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine as drug carriers for cancer therapy.
abstract: Novel amphiphilic copolymer nanoparticles (HPAE-co-PLA-DPPE) composed of hyperbranched poly (amine-ester), polylactide and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) segments were designed and synthesized that provided high encapsulation efficiency. These nanoparticles (NPs) were used to encapsulate an antitumor model drug, doxorubicin (DOX). The resulting NPs exhibited high encapsulation efficiency to DOX under an appropriate condition. In vitro release experiments revealed that the release of DOX from NPs was faster at pH 4.5 than that at pH 7.4 or pH 6.0. Confocal microscopy observation indicated that the DOX-loaded NPs can enter cells and localize in lysosomes that can be released quickly into the cytoplasm. The DOX-loaded NPs showed comparable anticancer efficacy with the free drug both in vivo and in vitro. These results demonstrate a feasible application of the hyperbranched copolymer, HPAE-co-PLA-DPPE, as a promising nanocarrier for intracellular delivery of antitumor drugs.
  
  
  BACKGROUND
  In this paper, the development of novel amphiphilic copolymer nanoparticles is discussed with the goal of establishing high encapsulation efficiency for chemotherapy drugs.
authors.affiliation: CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Beijing, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wu
authors.forename: Fang
authors.initials: F
authors.lastname: Jiao
authors.forename: Siyuan
authors.initials: S
authors.lastname: Han
authors.forename: Tengfei
authors.initials: T
authors.lastname: Fan
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.forename: Liming
authors.initials: L
authors.lastname: Hu
authors.forename: Yuliang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Chunying
authors.initials: C
authors.lastname: Chen
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000627:therapeutic use; D005260:Female; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy; D010714:Phosphatidylethanolamines / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D010714:Phosphatidylethanolamines; C007510:1,2-dipalmitoyl-3-phosphatidylethanolamine; D004317:Doxorubicin