Targetted Delivery of Doxorubicin into Human Liver Cancer Cells Encapsulated with D-Galactose-Peptide Amphiphile

Liver cancer cells have been reported to have an over-expression of asialoglycoprotein receptor, which were able to recognize D-galactose residue. In this study, we have designed and synthesize an amphiphilic peptide-galactose conjugate to self-assemble into core-shell micelle nanoparticle with a small hydrodynamic radius of around 200nm. The micelle was used to encapsulate anticancer drug, doxorubicin, as a model drug. Encapsulation efficiency, loading level, and in vitro release profile of the peptide-galactose conjugate was studied as a novel and non-cytotoxic carrier of drugs to target cells with over-expression of asialoglycoprotein receptors. To evaluate the targeting capability of this carrier, cytotoxicity study of doxorubicin-loaded into D-galactose-peptide conjugate was performed against human liver carcinoma, HepG2 cell lines, under competitive binding with free D-Galactose present in the culture media. As a control study, we had also provided similar experiments against human breast cancer, PC3 cell lines, which does not have an over-expression of glycoprotein receptors.