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Preparation, Characterization, and In Vitro and In Vivo Evaluation of PEGylated Liposomal Doxorubicin Modified with Different cRGD Peptides

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Part of the book series: Methods in Pharmacology and Toxicology ((MIPT))

Abstract

Liposomes containing cytotoxic agents and decorated with Cyclic Arg-Gly-Asp (cRGD) pentapeptides have attracted considerable attention for targeting tumor vasculature. These cRGD peptides have been used for targeting liposomes or other nano-carriers to inflamed or tumoral tissues; however, no comparative study dealing with the biological performances of liposomes decorated with different cRGDs could be found in the literature.

Herein, we prepared PEGylated Liposomal Doxorubicin (PLD) conjugated with different three cRGD peptides (RGD-PLDs). RADyC-PLD and not modified PLDs (Plain-PLD) were prepared as negative controls. Then, all the preparations were comparatively evaluated with respect to their in vitro behaviors (cell interactions and cytotoxicity) and in vivo performances (biodistribution and therapeutic efficacy) in tumored mice.

In this chapter, we present the general flowchart applied for this project as follow: (1) preparation of peptide-modified PLDs, (2) characterization of colloidal properties and stability of PLDs, (3) in vitro cell interaction and cytotoxicity, and (4) in vivo biodistribution and therapeutic efficacy in mice bearing C-26 colon carcinoma tumor model.

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Correspondence to Mahmoud Reza Jaafari .

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Amin, M., Jaafari, M.R. (2015). Preparation, Characterization, and In Vitro and In Vivo Evaluation of PEGylated Liposomal Doxorubicin Modified with Different cRGD Peptides. In: Patsenker, E. (eds) Integrin Targeting Systems for Tumor Diagnosis and Therapy. Methods in Pharmacology and Toxicology. Humana Press, New York, NY. https://doi.org/10.1007/7653_2015_57

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  • DOI: https://doi.org/10.1007/7653_2015_57

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  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-7443-6

  • Online ISBN: 978-1-4939-7445-0

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