Preparation and in vitro evaluation of GalNac-modified liposomes containing coumarin 6

NIE Hua; YANG Qi-xuan; ZHAO Ying; YE Xiao-ling; ZHONG Yu-bo; LI Zhuo-lin; ZHANG Sheng-yuan

Abstract：Objective:To construct the N-acetylgalactosamine (GalNAc)-modified liposomes as the carriers of coumarin 6 by enzymatic method and evaluate its physicochemical property.Methods:The GalNAc-C8-Chol was synthesized by enzyme catalysis.The structure characterization of the product was confirmed by MS and NMR.The GalNAc-C8-Chol-modified coumarin 6-loaded liver targeting liposomes (NGAL-LP) were prepared by thin film dispersion-extrusion method.The encapsulation efficiency,particle size,Zeta potential and in vitro drug release of NGAL-LP were investigated.The in vitro lectin-induced aggregation of NGAL-LP was evaluated using Ricinus communis agglutinin (RCA120) assay.Results:The encapsulation efficiency of NGAL-LP was above 98％ and the modification of GalNAc-C8-Chol didn't affect its physicochemical characteristics,such as particle size,Zeta potential,encapsulation efficiency and in vitro drug release.The average size and Zeta potential of NGAL-LP were (86.74 ± 1.7)nm and (-51.47 ± 0.9) mV,respectively.There was no obvious difference in the in vitro release of coumarin 6 between the LP and NGAL-LP,which were both below 8％.RCA assay revealed enhanced aggregation of NGAL-LP compared to LP,confirming the presence of galactose on the surface of NGAL-LP.Conclusion:NGAL-LP was constructed successfully by enzymatic method and could be a potential formulation for targeted therapy of liver cancer.