Study on Preparation and in vitro Anticancer Activity of PFV-modified Paclitaxel/artesunate Co-loaded Targeting Micelles
- VernacularTitle:细胞穿膜肽PFV修饰紫杉醇/青蒿琥酯共载靶向胶束的制备及体外抗肿瘤作用研究
- Author:
Wei WANG
1
;
Xuetao LI
1
;
Liang KONG
1
;
Shuang JIANG
2
;
Yifu LUO
2
;
Xiaobo WANG
1
Author Information
1. School of Pharmacy，Liaoning University of TCM，Liaoning Dalian 116600，China
2. No. 967 Hospital of the Joint Logistic Support Force of PLA，Liaoning Dalian 116011，China
- Publication Type:Journal Article
- Keywords:
Cell-penetrating peptide;
Paclitaxel;
Micelles;
Artesunate;
Human gastric cancer BGC- 823 cells;
Targeting effects
- From:
China Pharmacy
2020;31(21):2592-2597
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE：To prepare cell penetrating peptide PFV-modified paclitaxel （PTX）/artesunate（ART）co-loaded targeting micelles ，and to investigate in vitro anti-tumor activity. METHODS ：According to optimal technology ，PFV-modified PTX/ ART co-loaded targeting micelles were prepared by membrane hydration method ，and were characterized. Using blank micelle as blank control ，sulforhodamine B （SRB）method was used to evaluate the toxicity of PTX micelles ，ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to human gastric cancer BGC- 823 cells. The coumarin was used as fluorescent probe replacing PTX to prepare corresponding micelles. Then ，the uptake of BGC- 823 cells to corresponding micelles and targeting effect were observed and determined by flow cytometry and fluorescence microscope. The effects of PTX micelles ， ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles on the invasion of BGC- 823 cells were investigated by Transwell chamber method. RESULTS ：Average particle size of PFV-modified PTX/ART co-loaded targeting micelles was （51.30±3.95）nm；PDI was 0.19±0.01，and Zeta potential was （0.21±0.02）mV. The encapsulation efficiency of PTX and ART were higher than 90％. The shape of micelles were spherical. The blank micelles had no obvious toxicity to BGC-823 cells. The IC 50 value of PTX micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to BGC-823 cells were （3.09±0.22），（1.93±0.24），（1.11±0.15）μmol/L，respectively. The distribution amount of different micelles in BGC- 823 cell nucleus in the descending order were PFV-modified coumarin/ART micelles ＞coumarin/ART micelles ＞coumarin micelles＞blank control. The order of inhibitory effect was PFV-modified PTX/ART co-loaded targeting micelles ＞PTX/ART micelles＞ART micelles ＞PTX micelles ＞blank control. CONCLUSIONS： Prepared PFV-modified PTX/ART No.81874347） co-loaded targeting micelles are in line with the quality of 1915286446@qq.com Chinese Pharmacopoeia . It shows strong cytotoxicity to BGC-823 cells，can improve the drug targeting and the cell uptake，and inhibit the inv asion and metastasis of BGC- 823 cells.
