Prescription Technology Optimization of RPV Modified Paclitaxel and Schisandrin B Liposomes and Preliminary Evaluation of Antitumor Activity in vitro / 中国药房

ABSTRACT

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 .