Preparation and evaluation of quality，targeting and cytotoxicity of triptolide-loaded targeting nanoparticles
- VernacularTitle:载雷公藤甲素靶向制剂的制备及质量、靶向性、细胞毒性评价
- Author:
Moli YIN
1
;
Wenbin LUO
1
;
Jingzhe XU
1
;
Zebo TANG
2
;
Ni GUO
3
;
Youxing LAO
1
;
Huiyan WANG
1
Author Information
1. Jilin Collaborative Innovation Center for Antibody Engineering，Jilin Medical University，Jilin Jilin 132013，China
2. College of Basic Medicine，Jilin Medical University，Jilin Jilin 132013，China
3. National-Local Joint Engineering Research Center of Biodiagnostics and Biotherapy，the Second Affiliated Hospital of Xi’an Jiaotong University，Xi’an 710299，China
- Publication Type:Journal Article
- Keywords:
triptolide;
rheumatoid arthritis;
cytotoxicity;
targeting preparation;
nanoparticles
- From:
China Pharmacy
2025;36(12):1457-1462
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To prepare nanoparticle-based targeting preparation loaded with triptolide （TP）， and evaluate its quality， targeting ability and cytotoxic effects. METHODS Polymer nanoparticles carrying TP-targeted folic acid （FA） receptor （TP@PLGA-PEG-FA） were fabricated using poly （lactic-co-glycolic acid）/polyethylene glycol/FA （PLGA-PEG-FA） as the carrier by emulsion and volatilization technique. The morphology and distribution were observed， and their particle size， Zeta potential， polydispersity index （PDI）， drug loading capacity and encapsulation efficiency were measured. Their stability， blood compatibility， in vitro drug release， uptake by RAW264.7 cells （localization with fluorescent dye Cy3.5）， and in vitro cytotoxicity were evaluated. RESULTS TP@PLGA-PEG-FA exhibited spherical shape and uniform distribution， with particle size of （122.60±0.02） nm， Zeta potential of （－17.6±0.6）mV， and PDI of 0.26±0.02； drug loading capacity and encapsulation efficiency of TP were measured to be （7.78±0.05）% and （68.62±0.03）%， respectively. The hemolysis rates of 100， 200， 300， 400 µg/mL TP@PLGA- PEG-FA were 0.77%， 0.92%， 1.34% and 1.63%， respectively. There were no significant changes in particle size， PDI and Zeta potential when TP@PLGA-PEG-FA were placed in 4 ℃ water for 14 days and in DMEM culture medium containing 10% fetal bovine serum at 37 ℃ for 12 h. The cumulative release rate of TP@PLGA-PEG-FA was （84.83±0.29）% in phosphate buffer at pH5.5 for 72 h， which was significantly higher than the cumulative release rates in phosphate buffer solutions at pH7.4 and 6.5 for 72 h （[ 42.37±0.35）% and （63.83±0.29）% ， respectively] （P＜0.05）. Activated RAW264.7 cells took up significantly more Cy3.5@PLGA-PEG-FA than they took up Cy3.5@PLGA-PEG-FA+free FA and Cy3.5@PLGA-PEG. When the mass concentration of TP was≥15.63 ng/mL， the survival rates of activated cells in the TP@PLGA-PEG-FA groups were significantly lower than those of the same mass concentration of free TP groups （P＜0.05）. CONCLUSIONS The prepared TP@PLGA-PEG-FA has high stability， good blood compatibility， active targeting and cytotoxicity to inflammatory cells.
