Study of Preparation and in Vitro Activity of Stearyl Alcohol Galactosidase Modified Axitinib Liposomes

OBJECTIVE To study presciption screening and in vitro activity of stearyl alcohol galactosidase modified Axitinib liposomes. METHODS Stearyl alcohol galactosidase modified axitinib liposomes were prepared with transmembrane ammonium sulfate gradients. Encapsulation efficiency and particle size were used as the evaluation index. The role of stearyl alcohol galactosidase modified axitinib liposomes in inducing proliferation and apoptosis of liver cancer SMMC-7721 cells was studied. The inhibitory effect of stearyl alcohol galactosidase modified Axitinib liposomes on growth of SMMC-7721 was tested by CCK-8 assay. Apoptosis of SMMC-7721 cells was assayed by Annexin V/PI flow cytometry. RESULTS The best prescription were as follows: the ratio of axitinib to phospholipids was 1∶14.95, the cholesterol and phospholipids ratio was 1∶4.45, the optimum temperature was 61.93 ℃, volume of ammonium sulfate solution was 4.31 mL. The diameter and entrapment efficiency were (252±6.4)nm and (68.50±0.85)%. The result of CCK-8 assay showed that the inhibition rate increased with time going on at the same drug concentration, the inhibition rate increased with the drug concentration increasing at the same time. The result of Annexin V/PI flow cytometry assay showed that the inhibition effect of stearyl alcohol galactosidase modified axitinib liposomes on SMMC-7721 cells were better than A549 under the same conditions. CONCLUSION The selected formulation and preparation technique of stearyl alcohol galactosidase modified axitinib liposomes with transmembrane ammonium sulfate gradients is reasonable and practicable. The axitinib liposomes modified by stearyl alcohol galactosidase have higher cytotoxicity to SMMC-7721 cells, and stronger apoptosis-inducing of SMMC-7721 than A549. The preliminary determination is made that stearyl alcohol galactosidase modified axitinib liposomes are of specific active hepatic targeting.