Document Type

Journal Article

Department/Unit

School of Chinese Medicine

Language

English

Abstract

A main hurdle for the success of tumor-specific liposomes is their inability to penetrate tumors efficiently. In this study, we incorporated a cell-penetrating peptide BR2 onto the surface of a liposome loaded with the anticancer drug cantharidin (CTD) to create a system targeting hepatocellular carcinoma (HCC) cells more efficiently and effectively. The in vitro cytotoxicity assay comparing the loaded liposomes’ effects on hepatocellular cancer HepG2 and the control Miha cells showed that CTD-loaded liposomes had a stronger anticancer effect after BR2 modification. The cellular uptake results of HepG2 and Miha cells further confirmed the superior ability of BR2-modified liposomes to penetrate cancer cells. The colocalization study revealed that BR2-modified liposomes could enter tumor cells and subsequently release drugs. A higher efficiency of delivery by BR2 liposomes as compared to unmodified liposomes was evident by evaluation of the HepG2 tumor spheroids penetration and inhibition. The biodistribution studies and anticancer efficacy results in vivoshowed the significant accumulation of BR2-modified liposomes into tumor sites and an enhanced tumor inhibition. In conclusion, BR2-modified liposomes improve the anticancer potency of drugs for HCC.

Keywords

Cell penetrating peptides, cancer cell specific peptide BR2, cantharidin, hepatocellular carcinoma, liposome drug delivery system

Publication Date

2017

Source Publication Title

Drug Delivery

Volume

24

Issue

1

Start Page

986

End Page

998

Publisher

Taylor & Francis

DOI

10.1080/10717544.2017.1340361

Link to Publisher's Edition

https://doi.org/10.1080/10717544.2017.1340361

ISSN (print)

10717544

ISSN (electronic)

15210464

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