title: Solid lipid nanoparticles by coacervation loaded with a methotrexate prodrug: preliminary study for glioma treatment.
abstract: OBJECTIVE
  Methotrexate-loaded biocompatible nanoparticles were tested for preliminary efficacy in glioma treatment.
  
  
  METHODS
  Behenic acid nanoparticles, prepared by the coacervation method, were loaded with the ester prodrug didodecylmethotrexate, which was previously tested in vitro against glioblastoma human primary cultures. Nanoparticle conjugation with an ApoE mimicking chimera peptide was performed to obtain active targeting to the brain.
  
  
  CONCLUSIONS
  Biodistribution studies in healthy rats assessed the superiority of ApoE-conjugated formulation, which was tested on an F98/Fischer glioma model. Differences were observed in tumor growth rate (measured by MRI) between control and treated rats. In vitro tests on F98 cultured cells assessed their susceptibility to treatment, with consequent apoptosis, and allowed us to explain the apoptosis observed in glioma models.
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Battaglia
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Muntoni
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Chirio
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Peira
authors.affiliation: Centro Ricerche di Neurobiooncologia, Policlinico di Monza Foundation, Vercelli, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Annovazzi
authors.affiliation: Centro Ricerche di Neurobiooncologia, Policlinico di Monza Foundation, Vercelli, Italy.
authors.forename: Davide
authors.initials: D
authors.lastname: Schiffer
authors.affiliation: Centro Ricerche di Neurobiooncologia, Policlinico di Monza Foundation, Vercelli, Italy.
authors.forename: Marta
authors.initials: M
authors.lastname: Mellai
authors.affiliation: Dipartimento di Oncologia, Università degli Studi di Torino, Orbassano, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Riganti
authors.affiliation: Dipartimento di Oncologia, Università degli Studi di Torino, Orbassano, Italy.
authors.forename: Iris Chiara
authors.initials: IC
authors.lastname: Salaroglio
authors.affiliation: Dipartimento di Neuroscienze, Università degli Studi di Torino, Torino, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Lanotte
authors.affiliation: Dipartimento di Neuroscienze, Università degli Studi di Torino, Torino, Italy.
authors.forename: Pierpaolo
authors.initials: P
authors.lastname: Panciani
authors.affiliation: Dipartimento di Scienze Veterinarie, Università degli Studi di Torino, Grugliasco, Italy.
authors.forename: Maria Teresa
authors.initials: MT
authors.lastname: Capucchio
authors.affiliation: Dipartimento di Scienze Veterinarie, Università degli Studi di Torino, Grugliasco, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Valazza
authors.affiliation: Dipartimento di Scienze Veterinarie, Università degli Studi di Torino, Grugliasco, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Biasibetti
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.
authors.forename: Marina
authors.initials: M
authors.lastname: Gallarate
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D005910:Glioma / Q000188:drug therapy*; D006801:Humans; D008055:Lipids / Q000008:administration & dosage / Q000737:chemistry; D008727:Methotrexate / Q000008:administration & dosage* / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D008055:Lipids; D011355:Prodrugs; D008727:Methotrexate
keywords: ApoE; apoptosis; biodistribution; chimera peptide; coacervation; glioma; methotrexate; orthotopic model; solid lipid nanoparticles