Research Papers:

A nanostructure of functional targeting epirubicin liposomes dually modified with aminophenyl glucose and cyclic pentapeptide used for brain glioblastoma treatment

Cheng-Xiang Zhang _, Wei-Yu Zhao, Lei Liu, Rui-Jun Ju, Li-Min Mu, Yao Zhao, Fan Zeng, Hong-Jun Xie, Yan Yan and Wan-Liang Lu

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Oncotarget. 2015; 6:32681-32700. https://doi.org/10.18632/oncotarget.5354

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Cheng-Xiang Zhang1, Wei-Yu Zhao1, Lei Liu1, Rui-Jun Ju1, Li-Min Mu1, Yao Zhao1, Fan Zeng1, Hong-Jun Xie1, Yan Yan1, Wan-Liang Lu1

1Beijing Key Laboratory of Molecular Pharmaceutics and New Drug System, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

Correspondence to:

Wan-Liang Lu, e-mail: [email protected]

Keywords: Functional targeting epirubicin liposomes, BBB, brain glioblastoma, neovasculatures, mechanism and efficacy

Received: April 14, 2015     Accepted: September 14, 2015     Published: September 25, 2015


The objectives of the present study were to develop functional targeting epirubicin liposomes for transferring drugs across the blood-brain barrier (BBB), treating glioblastoma, and disabling neovascularization. The studies were performed on glioblastoma cells in vitro and on glioblastoma-bearing mice. The results showed that the constructed liposomes had a high encapsulation efficiency for drugs (>95%), suitable particle size (109 nm), and less leakage in the blood component-containing system; were significantly able to be transported across the BBB; and exhibited efficacies in killing glioblastoma cells and in destroying glioblastoma neovasculature in vitro and in glioblastoma-bearing mice. The action mechanisms of functional targeting epirubicin liposomes correlated with the following features: the long circulation in the blood system, the ability to be transported across the BBB via glucose transporter-1, and the targeting effects on glioblastoma cells and on the endothelial cells of the glioblastoma neovasculature via the integrin β3 receptor. In conclusion, functional targeting epirubicin liposomes could be used as a potential therapy for treating brain glioblastoma and disabling neovascularization in brain glioblastomas.

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