Liposomes for PET and MR Imaging and for Dual Targeting (Magnetic Field/Glucose Moiety): Synthesis, Properties, and in Vivo Studies

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• 作者：Jérémy Malinge ; Bastien Géraudie ; Paul Savel ; Valérie Nataf ; Aurélie Prignon ; Claire Provost ; Yongmin Zhang ; Phalla Ou ; Khaldoun Kerrou ; Jean-Noël Talbot ; Jean-Michel Siaugue ; Matthieu Sollogoub ; Christine Ménager
• 刊名：Molecular Pharmaceutics
• 出版年：2017
• 出版时间：February 6, 2017
• 年：2017
• 卷：14
• 期：2
• 页码：406-414
• 全文大小：611K
• ISSN：1543-8392

文摘

We describe the potentiality of a new liposomal formulation enabling positron emission tomography (PET) and magnetic resonance MR() imaging. The bimodality is achieved by coupling a ⁶⁸Ga-based radiotracer on the bilayer of magnetic liposomes. In order to enhance the targeting properties obtained under a permanent magnetic field, a sugar moiety was added in the lipid formulation. Two new phospholipids were synthesized, one with a specific chelator of ⁶⁸Ga (DSPE-PEG-NODAGA) and one with a glucose moiety (DSPE-PEG-glucose). The liposomes were produced according to a fast and safe process, with a high radiolabeling yield. MR and PET imaging were performed on mice bearing human glioblastoma tumors (U87MG) after iv injection. The accumulation of the liposomes in solid tumor is evidenced by MR imaging and the amount is evaluated in vivo and ex vivo according to PET imaging. An efficient magnetic targeting is achieved with these new magnetic liposomes.