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Open AccessArticle

Anticancer Efficacy of Targeted Shikonin Liposomes Modified with RGD in Breast Cancer Cells

Public Health College, Harbin Medical University, Harbin 150081, China
Research Institute of Medicine & Pharmacy, Qiqihar Medical University, Qiqihar 161006, China
Author to whom correspondence should be addressed.
Molecules 2018, 23(2), 268;
Received: 2 January 2018 / Revised: 22 January 2018 / Accepted: 26 January 2018 / Published: 29 January 2018
(This article belongs to the Special Issue Liposomes as Drug Carriers)
PDF [3863 KB, uploaded 29 January 2018]


Shikonin (SHK) has been proven to have a good anti-tumor effect. However, poor water solubility and low bioavailability limit its wide application in clinical practice. In this study, to overcome these drawbacks, RGD-modified shikonin-loaded liposomes (RGD-SSLs-SHK) were successfully prepared. It exhibited excellent physicochemical characteristics including particle size, zeta potential, encapsulation efficiency, and delayed release time. Meanwhile, the targeting activity of the RGD-modified liposomes was demonstrated by flow cytometry and confocal microscopy in the αvβ3-positive MDA-MB-231 cells. Besides exhibiting greater cytotoxicity in vitro, compared with non-targeted shikonin-loaded liposomes (SSLs-SHK), RGD-SSLs-SHK could also evidently induce apoptosis by decreasing the expression of Bcl-2 and increasing the expression of Bax. It could also inhibit cell proliferation, migration, invasion, and adhesion by reducing the expression of MMP-9 and the level of NF-κB p65, but did not affect the expression of MMP-2 in the MDA-MB-231 cells. Therefore, these findings indicated that the strategy to use RGD-modified liposomes as carriers for targeted delivery of shikonin is a very promising approach to achieve breast cancer targeted therapy. View Full-Text
Keywords: shikonin; integrin αvβ3; liposomes; apoptosis; migration; targeted therapy shikonin; integrin αvβ3; liposomes; apoptosis; migration; targeted therapy

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Wen, X.; Li, J.; Cai, D.; Yue, L.; Wang, Q.; Zhou, L.; Fan, L.; Sun, J.; Wu, Y. Anticancer Efficacy of Targeted Shikonin Liposomes Modified with RGD in Breast Cancer Cells. Molecules 2018, 23, 268.

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