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Preparation and evaluation of RGD and TAT co-modified docetaxel-loaded liposome

Authors Zhu R, Tian Y

Received 21 August 2017

Accepted for publication 5 October 2017

Published 6 December 2017 Volume 2017:11 Pages 3481—3489

DOI https://doi.org/10.2147/DDDT.S149620

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Akshita Wason

Peer reviewer comments 2

Editor who approved publication: Dr Anastasios Lymperopoulos

Ren Zhu,1,2 Ye Tian1,3

1Department of Radiotherapy and Oncology, The Second Affiliated Hospital of Soochow University, Suzhou, 2Department of Oncology, Shanghai Pulmonary Hospital, Tongji University School of Medicine, Shanghai, 3Institute of Radiotherapy and Oncology, Soochow University, Suzhou, People’s Republic of China

Abstract: The aim of this study is to develop a novel RGD and TAT co-modified docetaxel (DTX)-loaded liposome (LP) by the emulsification-solvent evaporation method. The prepared LPs were found to be in the size of 100 nm–110 nm. The transmission electron microscope photomicrographs were smooth, sub-spherical in shape, and aggregated to form small clusters. The DTX cumulative release from TAT and RGD co-modified LPs was significantly higher than that from other LPs due to decreased diffusion distance. Results of cell uptake showed that surface modification could indicate when cell internalization was changed and more drugs entered the cells successfully. Surprisingly, TAT and RGD co-modified DTX-LPs demonstrated a superior antiproliferative effect on A549 cells with a possible mechanism that suppressed the multidrug resistance phenomenon and exhibited a clear synergistic effect. In antitumor study, our results indicated that the form of TAT and RGD co-modified LPs had a better antitumor effect in vivo than the other formulations.

Keywords: RGD, TAT, liposome, cell uptake, cytotoxicity, antitumor

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