Preparation of paclitaxel-loaded and folic acid-modified poly (lactic-co-glycolic acid) nano-micelles and in vitro anticancer effect on cervical cancer HeLa cells.
10.19540/j.cnki.cjcmm.20210302.303
- Author:
Xin-Jian LI
1
;
Yun YOU
1
;
Qiong-Ling ZHANG
1
;
Bing-Bing ZHANG
1
;
Lin YAN
2
;
Ze-Min OU
1
;
Yao ZHANG
3
;
Yan-Jing WANG
3
;
Yan TONG
1
;
De-Wen LIU
1
;
Jin-Yu WANG
1
Author Information
1. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China.
2. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China School of Pharmacy, Jiangxi University of Traditional Chinese Medicine Nanchang 330004, China.
3. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine Tianjin 300193, China.
- Publication Type:Journal Article
- Keywords:
HeLa cells;
PLGA nano-micelles;
cellular uptake;
folic acid-mediated targeting
- MeSH:
Antineoplastic Agents, Phytogenic/pharmacology*;
Cell Line, Tumor;
Drug Carriers;
Female;
Folic Acid;
Glycolates;
HeLa Cells;
Humans;
Micelles;
Paclitaxel;
Particle Size;
Uterine Cervical Neoplasms/drug therapy*
- From:
China Journal of Chinese Materia Medica
2021;46(10):2481-2488
- CountryChina
- Language:Chinese
-
Abstract:
The paclitaxel-loaded and folic acid-modified poly(lactic-co-glycolic acid) nano-micelles(PTX@FA-PLGA-NMs) were prepared by the emulsion solvent evaporation method, and the parameters of paclitaxel-loaded nano-micelles were optimized with the particle size and PDI as evaluation indexes. The morphology of the nano-micelles was observed by transmission electron microscopy(TEM), and the stability, drug loading and encapsulation efficiency were systematically investigated. In vitro experiments were performed to study the cytotoxic effects of nano-micelles, apoptosis, and cellular uptake. Under the optimal parameters, the nano-micelles showed the particle size of(125.3±1.2) nm, the PDI of 0.086±0.026, the zeta potential of(-20.0±3.8) mV, the drug loading of 7.2%±0.75%, and the encapsulation efficiency of 50.7%±1.0%. The nano-micelles were in regular spherical shape as observed by TEM. The blank FA-PLGA-NMs exhibited almost no inhibitory effect on the proliferation and growth of tumor cells, while the drug-loaded nano-micelles and free PTX exhibited significant inhibitory effects. The IC_(50) of PTX@FA-PLGA-NMs and PTX was 0.56 μg·mL~(-1) and 0.66 μg·mL~(-1), respectively. The paclitaxel-loaded nano-micelles were potent in inhibiting cell migration as assessed by the scratch assay. PTX@FA-PLGA-NMs had good pro-apoptotic effect on cervical cancer HeLa cells and significantly promoted the uptake of HeLa cells. The results of in vitro experiments suggested that PTX@FA-PLGA-NMs could target and treat cervical cancer HeLa cells. Therefore, as nanodrug carriers, PTX@FA-PLGA-NMs with anti-cancer activity are a promising nano-system for improving the-rapeutic effects on tumors.
