Targeted Delivery of Cordycepin to Liver Cancer Cells Using Transferrin-conjugated Liposomes.
Bi YE, Zhou Y, Wang M, Li L, Lee RJ, Xie J, Teng L
Anticancer Res 37 5207-5214 01/01/2017
BACKGROUND/AIM: Cordycepin is an endogenous nucleoside with significant anticancer biological activity. The objective of this study was to develop targeted liposomes to improve solubility and biological activity of cordycepin.
MATERIALS AND METHODS: We established transferrin-conjugated liposomes to deliver cordycepin to liver cancer cells and evaluated the uptake and effect.
RESULTS: The liposomes were loaded with cordycepin. Their average size was 125.3 nm, with drug encapsulation efficiency of 65.3%. The liposomes had good colloidal stability and released cordycepin slowly. Liposomal cordycepin was shown to increase reactive oxygen species production and cause depolarization of the mitochondrial transmembrane in liver cancer cells. Cellular uptake of liposomal cordycepin was enhanced by conjugation to transferrin, that facilitated receptor-mediated endocytosis.
CONCLUSION: Transferrin-conjugated liposomes are effective as nanocarriers for cordycepin delivery to liver cancer cells.