Synthesis of cholesterol-based neoglycoconjugates and their use in the preparation of liposomes for active liver targeting

Abstract

Carbohydrate receptors on liver represent attractive targets for receptor-mediated delivery of nanostructured therapeutics. In this study, two new cholesterol-based glycoconjugates derived from d-galactose and N-acetylglucosamine were synthesized and incorporated into liposomes. ^99mTc-Cholesterol-DTPA complex was used for radiolabeling experiments in vivo with high radiochemical yields and stability. Biodistribution studies confirmed the targeting of galactosylated liposomes (GalL) to liver cells. These results indicated that GalL could be considered a promising drug delivery system for liver diseases therapy.

Keywords: Cholesterol-DTPA; Liposome; Liver targeting; Neoglycoconjugates; Sugar-binding receptor.