Anticancer Efficacy of Targeted Shikonin Liposomes Modified with RGD in Breast Cancer Cells
AbstractShikonin (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
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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.
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(2):268.Chicago/Turabian Style
Wen, Xianchun; Li, Jiping; Cai, Defu; Yue, Liling; Wang, Qi; Zhou, Li; Fan, Li; Sun, Jianwen; Wu, Yonghui. 2018. "Anticancer Efficacy of Targeted Shikonin Liposomes Modified with RGD in Breast Cancer Cells." Molecules 23, no. 2: 268.
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