Study on the enzyme-catalyzed synthesis of ligands for ASGPR-mediated liver targeting liposomes
- Author:
Bo-Hong GUO
1
Author Information
1. School of Pharmacy
- Publication Type:Journal Article
- Keywords:
Asialoglycoprotein receptor;
Enzyme-catalyzed;
Ligand;
Stearamine
- From:
Chinese Pharmaceutical Journal
2012;47(1):40-43
- CountryChina
- Language:Chinese
-
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.
