Target-selective drug delivery through liposomes labeled with oligobranched neurotensin peptides (Articolo in rivista)

Type
Label
  • Target-selective drug delivery through liposomes labeled with oligobranched neurotensin peptides (Articolo in rivista) (literal)
Anno
  • 2011-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1002/cmdc.201000463 (literal)
Alternative label
  • Falciani C, Accardo A, Brunetti J, Tesauro D, Lelli B, Pini A, Bracci L, Morelli G. (2011)
    Target-selective drug delivery through liposomes labeled with oligobranched neurotensin peptides
    in ChemMedChem (Internet)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Falciani C, Accardo A, Brunetti J, Tesauro D, Lelli B, Pini A, Bracci L, Morelli G. (literal)
Pagina inizio
  • 678 (literal)
Pagina fine
  • 685 (literal)
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  • 6 (literal)
Rivista
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  • 8 (literal)
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  • 4 (literal)
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  • Laboratory of Molecular Biotechnology, Department of Molecular Biology, University of Siena, Via Fiorentina 1, 53100 Siena, Italy. Istituto di Biostrutture e Bioimmagini - CNR,NAPOLI (literal)
Titolo
  • Target-selective drug delivery through liposomes labeled with oligobranched neurotensin peptides (literal)
Abstract
  • The structure and the in vitro behavior of liposomes filled with the cytotoxic drug doxorubicin (Doxo) and functionalized on the external surface with a branched moiety containing four copies of the 8-13 neurotensin (NT) peptide is reported. The new functionalized liposomes, DOPC-NT?Lys(C??)?, are obtained by co-aggregation of the DOPC phospholipid with a new synthetic amphiphilic molecule, NT? Lys(C??)?, which contains a lysine scaffold derivatized with a lipophilic moiety and a tetrabranched hydrophilic peptide, NT8-13, a neurotensin peptide fragment well known for its ability to mimic the neurotensin peptide in receptor binding ability. Dynamic light scattering measurements indicate a value for the hydrodynamic radius (RH) of 88.3±4.4 nm. The selective internalization and cytotoxicity of DOPC-NT? Lys(C??)? liposomes containing Doxo, as compared to pure DOPC liposomes, were tested in HT29 human colon adenocarcinoma and TE671 human rhabdomyosarcoma cells, both of which express neurotensin receptors. Peptide-functionalized liposomes show a clear advantage in comparison to pure DOPC liposomes with regard to drug internalization in both HT29 and TE671 tumor cells: FACS analysis indicates an increase in fluorescence signal of the NT?-liposomes, compared to the DOPC pure analogues, in both cell lines; cytotoxicity of DOPC-NT? Lys(C??)?-Doxo liposomes is increased four-fold with respect to DOPC-Doxo liposomes in both HT29 and TE671 cell lines. These effects could to be ascribed to the higher rate of internalization for DOPC-NT? Lys(C??)?-Doxo liposomes, due to stronger binding driven by a lower dissociation constant of the NT?-liposomes that bind the membrane onto a specific protein, in contrast to DOPC liposomes, which approach the plasma membrane unselectively. (literal)
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