Study on the enzyme-catalyzed synthesis of ligands for ASGPR-mediated liver targeting liposomes / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize asialoglycoprotein receptor ligand-targeted modifier which is used to insert the surface of liposome by enzyme-catalyzed amidation of lactobionic acid and stearamine. METHODS: The structure of the product was confirmed by IR, ESI-MS and H1-NMR. The effects of types and quantity of enzyme, organic solvents, molar ratio of substrate and temperature of reaction were studied. RESULTS: When using DMSO as reaction medium, Novozym 435 immobilized lipase at 400 U · mL-1, molar ratio of lactobionic acid to stearamine at 2:1, and reacting at 40°C for 24 h, the transformation of stearamine reached more than 99%. CONCLUSION: The enzyme catalysis is useful for synthesizing liver targeting liposomes.