Comparison of tumor neovasculature-targeted paramagnetic nanoliposomes for MRI in mice xenograft models

• Autores: Q.-H. Xu, J.-Y. Shi, J. Zhang, Y.-F. Sun, A. H. Chang, Y.-M. Zhao, W.-J. Cai, D. Liu, C.-C. Zhou, L.-H. Fan, B. Su
• Localización: Clinical & translational oncology, ISSN 1699-048X, Vol. 16, Nº. 4, 2014, págs. 395-401
• Idioma: inglés
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• Resumen

  • Introduction 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 ?v?3 and VEGFR-1, VEGFR-2, respectively, and compared their potential value as MRI contrast agents for detecting small tumors in animal models.

    Materials and 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 × 107, 6.01 × 107, and 3.85 × 107 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.

    Conclusion RGD10 and K237 targeted paramagnetic nanoliposomes can be developed as potential tumor-specific MRI contrast agents and are helpful for tumor detection.