title: Comparison of tumor neovasculature-targeted paramagnetic nanoliposomes for MRI in mice xenograft models.
abstract: BACKGROUND
  Neovasculature imaging is a promising approach for tumor diagnosis. We constructed tumor neovasculature targeted paramagnetic nanoliposomes with RGD10, F56, and K237 peptides, which can bind to Integrin αvβ3 and VEGFR-1, VEGFR-2, respectively, and compared their potential value as MRI contrast agents for detecting small tumors in animal models.
  
  
  METHODS
  Peptide-Ahx-palmitic acid conjugate was synthesized using Fmoc solid-phase synthesis chemistry. Targeted paramagnetic nanoliposomes were prepared by the thin film dispersion-sonication method. The tumor signal enhancements of liposome particles were evaluated by MRI in a xenograft mice model.
  
  
  RESULTS
  The apparent affinity constants of RGD10, K237, and F56 peptides binding to their cell receptors were 9.15 × 10(7), 6.01 × 10(7), and 3.85 × 10(7) mol/L, respectively. RGD10 and K237 targeted paramagnetic nanoliposomes have shown much greater tumor-specific MRI signal enhancement in xenograft of the nude mice compared to F56 targeted paramagnetic nanoliposome. Tumor signal enhancement rate (SER %) increased 2.21 ± 0.09 and 1.82 ± 0.05 fold, respectively, for RGD10 and K237 compared to non-targeted control in T1 weighted MR image.
  
  
  CONCLUSIONS
  RGD10 and K237 targeted paramagnetic nanoliposomes can be developed as potential tumor-specific MRI contrast agents and are helpful for tumor detection.
authors: Department of Oncology, Shanghai Pulmonary Hospital, Tongji University School of Medicine, Shanghai, 200433, China.
authors: Q-H
authors: QH
authors: Xu
authors: J-Y
authors: JY
authors: Shi
authors: J
authors: J
authors: Zhang
authors: Y-F
authors: YF
authors: Sun
authors: A H
authors: AH
authors: Chang
authors: Y-M
authors: YM
authors: Zhao
authors: W-J
authors: WJ
authors: Cai
authors: D
authors: D
authors: Liu
authors: C-C
authors: CC
authors: Zhou
authors: L-H
authors: LH
authors: Fan
authors: B
authors: B
authors: Su
mesh_terms: D000818:Animals; D003952:Diagnostic Imaging / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D008081:Liposomes; D008279:Magnetic Resonance Imaging / Q000379:methods*; D008297:Male; D053768:Metal Nanoparticles; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000473:pathology*; D009389:Neovascularization, Pathologic / Q000473:pathology; D023041:Xenograft Model Antitumor Assays
chemical_list: D008081:Liposomes
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