title: Efficacy and pharmacokinetics of a modified acid-labile docetaxel-PRINT(®) nanoparticle formulation against non-small-cell lung cancer brain metastases.
abstract: Particle Replication in Nonwetting Templates (PRINT(®)) PLGA nanoparticles of docetaxel and acid-labile C2-dimethyl-Si-Docetaxel were evaluated with small molecule docetaxel as treatments for non-small-cell lung cancer brain metastases.
  
  
  
  Pharmacokinetics, survival, tumor growth and mice weight change were efficacy measures against intracranial A549 tumors in nude mice. Treatments were administered by intravenous injection.
  
  
  
  Intracranial tumor concentrations of PRINT-docetaxel and PRINT-C2-docetaxel were 13- and sevenfold greater, respectively, than SM-docetaxel. C2-docetaxel conversion to docetaxel was threefold higher in intracranial tumor as compared with nontumor tissues. PRINT-C2-docetaxel increased median survival by 35% with less toxicity as compared with other treatments.
  
  
  
  The decreased toxicity of the PRINT-C2-docetaxel improved treatment efficacy against non-small-cell lung cancer brain metastasis.
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.
authors.forename: Maria
authors.initials: M
authors.lastname: Sambade
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.
authors.forename: Allison
authors.initials: A
authors.lastname: Deal
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Pharmacology, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Allison
authors.initials: A
authors.lastname: Schorzman
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.
authors.forename: J Christopher
authors.initials: JC
authors.lastname: Luft
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Chemistry, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Charles
authors.initials: C
authors.lastname: Bowerman
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Pharmacology, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Kevin
authors.initials: K
authors.lastname: Chu
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Medicine, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Olga
authors.initials: O
authors.lastname: Karginova
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.
authors.forename: Amanda Van
authors.initials: AV
authors.lastname: Swearingen
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Pharmacology, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: William
authors.initials: W
authors.lastname: Zamboni
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Chemistry, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Joseph
authors.initials: J
authors.lastname: DeSimone
authors.affiliation: Lineberger Comprehensive Cancer Center, Chapel Hill, NC, USA.|Department of Medicine, University of North Carolina, Chapel Hill, NC, USA.
authors.forename: Carey K
authors.initials: CK
authors.lastname: Anders
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000187:drug effects / Q000473:pathology; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000473:pathology / Q000556:secondary; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000473:pathology / Q000556:secondary; D045744:Cell Line, Tumor; D000077143:Docetaxel; D064593:Heterografts; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D053758:Nanoparticles / Q000737:chemistry*; D009368:Neoplasm Transplantation; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D043823:Taxoids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D043823:Taxoids; D000077143:Docetaxel; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: Particle Replication in Non-wetting Templates (PRINT)® PLGA nanoparticle; acid-labile docetaxel prodrug; blood–brain barrier