Liposomes derivatized with tetrabranched neurotensin peptidesvia click chemistry reactions

Abstract

Liposomes decorated with neurotensin tetramers are obtained by using a post-liposomal derivatization method in which a click-chemistry reaction between liposomes containing azido functions on the external surface, DOPC/(C18)₂-Peg9-N₃ (90/10), and branched neurotensin peptides modified for the presence of a CC triple-bond [(NT8-13)₄-alkyne] is performed. Results show that the post liposomal derivatization method is very efficient and that click-chemistry procedures are very attractive for nanoparticle functionalization. A structural characterization of liposomes has been performed by dynamic light scattering (DLS) measurements. The hydrodynamic radii of pure DOPC and mixed DOPC/(C18)₂-Peg9-N₃ and DOPC/(C18)₂-Peg-triazole-(NT8-13)₄ liposomes (at 90 : 10 molar ratio) are 61 ± 21 nm, 60 ± 22 nm and 82 ± 43 nm, respectively. A very efficient doxorubicin loading has been observed, specially for DOPC/(C18)₂-Peg9-N₃ liposomes, with a drug loading content of 90%.