Prescription Technology Optimization of RPV Modified Paclitaxel and Schisandrin B Liposomes and Preliminary Evaluation of Antitumor Activity in vitro
- VernacularTitle:RPV修饰的紫杉醇与五味子乙素脂质体处方工艺优化及体外抗肿瘤活性初步评价
- Author:
Lu ZHANG
1
;
Siyu HE
1
;
Xinze LIU
1
;
Liang KONG
1
;
Xuetao LI
1
Author Information
1. School of Pharmacy，Liaoning University of TCM，Liaoning Dalian 116600，China
- Publication Type:Journal Article
- Keywords:
Paclitaxel;
Schisandrin B;
Cell penetrating
- From:
China Pharmacy
2021;32(10):1173-1180
- CountryChina
- Language:Chinese
-
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 .
