RESUMEN
OBJECTIVE:To prepare paclit axel and schisandrin B liposomes modified by cell penetrating peptide RPV ,and to preliminarily evaluate its anti-tumor activity in vitro . METHODS :RPV modified paclitaxel and schisandrin B liposomes were prepared by film dispersion method. Box-Benhken design-response surface methodology was used to optimize the prescription technology of RPV modified paclitaxel and schisandrin B liposomes using the amount of cholesterol and paclitaxel ,the time interval of ultrasound probe as factors ,average entrapment efficiency of paclitaxel and schisandrin B was used as the index. The liposomes prepared by the optimal technology were characterized. Sulfonylrhodamine B staining method was used to investigate in vitro toxicity of RPV modified blank liposomes ,paclitaxel and schisandrin B liposomes ,RPV modified paclitaxel and schisandrin B liposomes to human ovarian cancer cell SK-OV- 3. The effects of 3 kinds of liposomes on the migration and invasion ability of SK-OV-3 cells were investigated by cell scratch test and Transwell chamber invasion test. RESULTS :The optimal prescription technology was phospholipid 44 mg,cholesterol 8 mg,paclitaxel 0.64 mg,schisandrin B 1.5 mg,ultrasonic probe time interval 5 s,prescription dosage 5 mL. According to the optimal prescription technology ,the liposomes were spherical in shape ,and the particle size was (126.49±1.19)nm,Zeta-potential was (-4.83±0.61)mV,average entrapment efficiency of liposomes was (93.88±1.67)%. Compared with RPV modified blank liposomes ,after treated with paclitaxel and schisandrin B liposomes and RPV modified paclitaxel and schisandrin B liposomes ,the survival rate ,migration inhibition rate and invasion rate of SK-OV- 3 cells were significantly decreased (P<0.05). The effects of RPV modified paclitaxel and schisandrin B liposomes was better than those of paclitaxel and schisandrin B liposomes (P<0.05). CONCLUSIONS :RPV modified paclitaxel and schisandra B liposome are successfu lly prepared ,and they have certain antitumor activity in vitro .