Effect of Cationic Liposome Formulation on Human Carcinoma Hepatic SMMC-7721 Cells' Uptake of Tenofovir and Cytotoxicity / 中国药房

ABSTRACT

OBJECTIVE:To investigate the effect of liposome formulation in promoting hepatocytes' uptake of tenofovir and cytotoxic effect. METHODS: The tenofovir cationic liposomes were prepared by tert-butyl lyophilization, and its encapsulation efficiency and physico-chemical property were determined. Using human hepatic carcinoma cells SMMC-7721 as a model to investigate the effect of liposome formulation in promoting hepatocytes' uptake of tenofovir. MTT assays were used to examine the toxicity of tenofovir cationic liposomes in different conditions. RESULTS: The prepared tenofovir cationic liposomes had an encapsulation efficiency of (88.3?1.6)%, a size distribution of (278.4?67.6)nm and a Zeta potential of (31?5)mV. The results showed that the liposome formulations containing galactose and PEG modifying lipids resulted in significantly higher and prolonged drug accumulation inside cells as compared with free drugs. The cell survival rates were above 80% when the tenofovir liposome was at a concentration of 7.5?g?mL-1 and lipids at a concentration of 30?g?mL-1, and little toxicity was noted. CONCLUSION: The prepared cationic liposome can greatly enhance hepatocytes' uptake and protection of tenofovir, which is expected to become a highly effective drug delivery system of antiviral drugs such as tenofovir etc.