title: Brain tumour targeting strategies via coated ferrociphenol lipid nanocapsules.
abstract: In this study, a new active targeting strategy to favour ferrociphenol (FcdiOH) internalisation into brain tumour cells was developed by the use of lipid nanocapsules (LNCs) coated with a cell-internalising peptide (NFL-TBS.40-63 peptide) that interacts with tubulin-binding sites. In comparison, OX26 murine monoclonal antibodies (OX26-MAb) targeting transferrin receptors were also inserted onto the LNC surface. The incorporation of OX26 or peptide did not influence the in vitro antiproliferative effect of FcdiOH-LNCs on the 9L cells since their IC50 values were found in the same range. In vivo, intracerebral administration of OX26-FcdiOH-LNCs or peptide-FcdiOH-LNCs by convection enhanced delivery did not enhance the animal median survival time in comparison with untreated rats (25 days). Interestingly, intra-carotid treatment with peptide-FcdiOH-LNCs led to an ameliorated survival time of treated rats with the presence of animals surviving until days 35, 40 and 44. Such results were not obtained with OX26-MAbs, demonstrating the benefit of NFL-TBS.40-63 peptide as an active ligand for peripheral drug delivery to the brain tumours.
authors.affiliation: Ingénierie de lVectorisation Particulaire in Micro et Nanomédecines Biomimétiques, LUNAM Université, Angers, France.
authors.forename: Anne-Laure
authors.initials: AL
authors.lastname: Laine
authors.forename: Ngoc Trinh
authors.initials: NT
authors.lastname: Huynh
authors.forename: Anne
authors.initials: A
authors.lastname: Clavreul
authors.forename: Julien
authors.initials: J
authors.lastname: Balzeau
authors.forename: Jérôme
authors.initials: J
authors.lastname: Béjaud
authors.forename: Anne
authors.initials: A
authors.lastname: Vessieres
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Benoit
authors.forename: Joël
authors.initials: J
authors.lastname: Eyer
authors.forename: Catherine
authors.initials: C
authors.lastname: Passirani
mesh_terms: D000818:Animals; D058846:Antibodies, Monoclonal, Murine-Derived / Q000008:administration & dosage / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001665:Binding Sites; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D016503:Drug Delivery Systems; D005260:Female; D005296:Ferrous Compounds / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D018316:Gliosarcoma / Q000188:drug therapy* / Q000473:pathology; D020128:Inhibitory Concentration 50; D008055:Lipids / Q000737:chemistry; D053769:Nanocapsules; D016900:Neurofilament Proteins / Q000737:chemistry; D010446:Peptide Fragments / Q000737:chemistry; D051381:Rats; D011916:Rats, Inbred F344; D011990:Receptors, Transferrin / Q000276:immunology; D015996:Survival Rate; D014404:Tubulin / Q000378:metabolism
chemical_list: D058846:Antibodies, Monoclonal, Murine-Derived; D000970:Antineoplastic Agents; D005296:Ferrous Compounds; D008055:Lipids; C576937:NFL-TBS.40-63 peptide; D053769:Nanocapsules; D016900:Neurofilament Proteins; D010446:Peptide Fragments; D011990:Receptors, Transferrin; D014404:Tubulin; C533771:ferrociphenol