Preparation of Norcantharidin Nano-micelle and Study on Its Antitumor Effect / 中国药房

ABSTRACT

OBJECTIVE:To prepare the norcantharidin (NCTD) nano-micelle and study its antitumor effect. METHODS:NCTD nano-micelle was self-formed in water using Triblock copolymers distearyl phosphatidylethanolamine-polyethylene glycol-ma-leimide;its shape was observed,the drug-loading rate,entrapment efficiency,particle size,Zeta potential were investigated. MTT was used to investigate the cell survival rate of human lung cancer A549 cells in negative control group (Phosphate buffer solu-tion),carrier group (blank nano-micelle),positive control group (NCTD APIs,5-320 μg/mL) and NCTD nano-micelle group (NCTD,5-320 μg/mL) after acting different time (24,48,72 h). Tumor nude mice were randomly divided into blank control group,NCTD injection group(1 mg/kg),NCTD low-dose,high-dose groups(0.5,1 mg/kg),6 in each group. All mice were in-travenously injected relevant medicines in tail,once a day,for 8 weeks. Tumor size was measured every week,and tumor quality was detected after the second day of finishing administration. RESULTS:NCTD nano-micelle was round,drug-loading rate was (2.82±0.05)%,entrapment efficiency was(83.67±1.78)%,particle size was(138.6±45.8)nm,Zeta potential was -(12.75± 0.34)mV(n=6). Cell survival rate of A549 cells in carrier group had no obvious changes,and was obviously decreased in posi-tive control group and NCTD nano-micelle group,which was positively correlated with concentration and time. And the decrease degree of cell survival rate in NCTD nano-micelle group was stronger than positive control group(P<0.01). Compared with blank control group,the tumor quality of mice in 3 administration groups was reduced (P<0.05),the reduction degree in NCTD na-no-micelle high-dose group was stronger than NCTD nano-micelle injection group (P<0.05). CONCLUSIONS:NCTD nano-mi-celle is successfully prepared,which has good in vitro and in vitro anti-tumor effect on A549 cells.