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Molecules 2018, 23(2), 268; doi:10.3390/molecules23020268

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

1
Public Health College, Harbin Medical University, Harbin 150081, China
2
Research Institute of Medicine & Pharmacy, Qiqihar Medical University, Qiqihar 161006, China
*
Author to whom correspondence should be addressed.
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)
View Full-Text   |   Download PDF [3863 KB, uploaded 29 January 2018]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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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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