Surface modification of liposomes for cardiomyocytes targeting in vitro.

The effect of novel 3-{4-[2-hydroxyl-(1-methyl ethylamine) propyl oxygen]phenyl}propionic acid cetylester (PAC) as a surface modification ligand on the delivery of liposomes into cultured cardiomyocytes was investigated. Small unilamellar liposomes with and without PAC (PAC-liposome and Plain-liposome) were labeled with a fluorescence marker. The cultured neonatal cardiomyocytes were incubated with liposomes under normoxia or hypoxia conditions, and then the cell-associated fluorescence was measured. A high affinity of the PAC-liposomes to cardiomyocytes was observed. The amount of cell uptake of PAC-liposomes under normoxia conditions was 4-fold higher than that of plain-liposome, and the increase was 8.5-fold when hypoxia occured. The results suggested that PAC is a potential surface modification ligand for liposome targeting the ischemic myocardium.