Yen Wah Tong, Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, Singapore, 117576, Singapore, Nikken Wiradharma, Drug Gene and Protein Delivery; Chemical and Biomolecular Engineering, Institute of Bioengineering and Nanotechnology; National University of Singapore, 31 Biopolis Way, #04-01, The Nanos, Singapore 138669, 21 Lower Kent Ridge Road, Singapore 119077, Singapore, Singapore, Shao Qiong Liu, Drug, Gene and Protein Delivery, Institute of Bioengineering and Nanotechnology, 31 Biopolis Way, #04-00, Singapore, 130889, Singapore, and Yi Yan Yang, Drugs, Proteins and Genes Delivery, Institute of Bioengineering and Nanotechnology, 31 Biopolis Way #04-01, Singapore, Singapore.
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.