关键词: T-2毒素, 脂质体, 薄膜超声法, 响应面法, 抗肿瘤活性

Abstract: T-2 toxin liposome (LPT2) was prepared by thin film ultrasonic method. Entrapment efficiency was determined by high performance liquid chromatography (HPLC) method, and the linearity, additive recovery, precision and repeatability of the method were investigated. Effects of organic solvent, phospholipid species, m(drug)∶m(lipid), hydration volume, m(phospholipids)∶m(cholesterol) on encapsulation efficiency were investigated by single factor method, and the prescription of T-2 toxin liposome was optimized by response surface method. The liposome was granulated by high pressure homogenization and particle size distribution was determined. The inhibitory effects of T-2 toxin and LPT2 on growth of 5 tumor cells and one normal cell were detected by thiazolyl blue (MTT) method. The results show that the best preparation process of LP-T2 are egg phosphatidylcholine (EPC) as membrance material, thin film ultrasonic method, m(drug)∶m(lipid)=3.5, m(phospholipid)∶m(cholesterol)=374, 4hydroxyethyl piperazine ethylsulfonic acid (Hepes， 20 mmol/L, pH=7.4) hydration, hydration volume 11.8 mL, ultrasound for 10 min. The average particle size after high pressure homogenization is 267 nm. LPT2 can significantly inhibit the proliferation of tumor cells, and its
 activity is similar to that of mitomycin. IC₅₀ value of normal cell (1 881.54 ng/mL) is higher than that of T2 toxin (1427.83 ng/mL). The entrapment efficiency and particle size of LPT2 conform to the standard of drug, and it has antitumor activity in vitro.

Key words: T-2 toxin, liposome, thin film ultrasonic method, response surface method, antitumor activity