ABSTRACT
Objective: Sialic acid (SA)-modified chlorogenic acid (CA) liposomes (CA-SAL) was prepared by response surface design to investigate its in vitro cytotoxicity and uptake. Methods: CA-SAL was prepared by a modified reverse-phase ethanol injection method. Sephadex G50 column was used to separate the CA-loaded liposomes and the free CA. The drug concentration was determined by HPLC method and the encapsulation efficiency was calculated. With encapsulation efficiency and drug loading as indicators, Box-Behnken response surface design experiments were used to optimize the prescription process of CA-SAL. The MTT method was used to evaluate the cytotoxicity of CA-SAL on human lung cancer cells A549. Inverted fluorescence microscope was used to investigate the uptake of CA-SAL by A549 cells. Results: The optimized preparation conditions: hydrogenated soybean lecithin-CA ratio at 15:1, hydration temperature 60 ℃, ultrasonic power 400 W. The average particle size of CA-SAL was (90.13 ± 0.51) nm, the polydispersity index (PDI) was 0.16 ± 0.01, the zeta potential was (-25.3 ± 0.5) mV, the encapsulation efficiency was 57.8%, RSD was 0.1%. MTT results showed that the inhibitory effect of CA-SAL on A549 cells was significantly greater than CA-CL. Greater cellular uptake of CA-SAL was observed compared with CA-CL. Conclusion: CA-SAL prepared by response surface optimization has a uniform particle size and good stability. SA-modified CA-loaded liposomes could enhance cellular uptake and cytotoxicity of human lung cancer cell A549 in vitro.