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Issue 45, 2018, Issue in Progress
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P1c peptide decorated liposome targeting αvβ3-expressing tumor cells in vitro and in vivo

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Abstract

Integrin αvβ3 is a promising target for integrin-rich tumor and neovascular. In the present study, we prepared a doxorubicin (DOX)-loaded liposome of which the surface was decorated with PEG and a novel αvβ3 targeting peptide of P1c. The in vitro targeting efficiency was evaluated in αvβ3-positive (U87MG) and -negative (MCF-7) tumor cells by flow cytometry and laser confocal scanning microscopy. The in vivo therapeutic effects were evaluated in the glioblastoma U87MG-tumor bearing mouse model. The results indicated that the prepared liposomes showed mean sizes of 131.2 and 128.4 nm in diameter for P1c-modified targeting liposomes (P1c-DOXL) and non-targeting liposomes (DOXL), respectively. The DOX encapsulation efficiencies were more than 95% in both types of liposomes. The conjugation ratio for P1c decoration was 66.8%. The flow cytometry and confocal laser-scanning microscopy experiments consistently showed that the intracellular fluorescence intensity of the P1c-modified targeted liposome group was stronger than that of the non-targeted liposome group (P < 0.05) in U87MG cells. In vivo results revealed that compared with DOX or DOXL treatment, P1c-DOXL dramatically reduced tumor growth (P < 0.05) and tumor angiogenesis while much lower hepatotoxicity was observed. P1c-modified targeting liposome exhibited sustained release, enhancing the antitumor effect of DOX through targeting tumor cells and neovascular where integrin αvβ3 was overexpressed. The results indicated that P1c might be promising for active targeting delivery in cancer therapy.

Graphical abstract: P1c peptide decorated liposome targeting αvβ3-expressing tumor cells in vitro and in vivo

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Publication details

The article was received on 11 Jun 2018, accepted on 08 Jul 2018 and first published on 18 Jul 2018


Article type: Paper
DOI: 10.1039/C8RA05014G
RSC Adv., 2018,8, 25575-25583
  • Open access: Creative Commons BY-NC license
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    P1c peptide decorated liposome targeting αvβ3-expressing tumor cells in vitro and in vivo

    W. Xu, X. Yan, N. Liu and G. Wu, RSC Adv., 2018, 8, 25575
    DOI: 10.1039/C8RA05014G

    This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

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