Preparation of Juglone-loaded PLGA Nanoparticles and Its Anti-tumor Effect on Melanoma A375 Cells in Vitro
10.13422/j.cnki.syfjx.20190114
- VernacularTitle: 胡桃醌-PLGA纳米粒制备及对A375恶黑细胞的体外抗肿瘤作用
- Author:
Wu-heng YUE
1
;
Rui MEI
1
;
Juan CAI
2
;
Han-qing QIAN
2
;
Bao-rui LIU
2
;
Zheng-yun ZOU
1
Author Information
1. Nanjing Drum Tower Hospital, Clinical College of Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210008, China
2. Nanjing Drum Tower Hospital, The Affiliated Hospital of Nanjing University Medical School, Nanjing 210008, China
- Publication Type:Research Article
- Keywords:
juglone;
poly lactic-co-glycolic acid (PLGA);
nanoparticles;
melanoma;
A375 cells
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2019;25(4):87-93
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To prepare Juglone-loaded poly lactic-co-glycolic acid nanoparticles (Jug-PLGA-NPs), and investigate their physicochemical properties, release characteristics in vitro and anti-tumor activities on A375 melanoma cells in vitro. Method: Jug-PLGA-NPs were prepared by emulsification-solvent evaporation method. Then the particle size, encapsulation efficiency, drug loading rate and in vitro release characteristics were investigated. Fluorescence microscopy was used to observe the uptake of PLGA-NPs in vitro. The distribution of PLGA-NPs in BALB/c nude mice after tail vein injection was observed by the small living animal imaging system. Their inhibition effect on proliferation of A375 cells was detected by thiazolyl blue tetrazolium bromide (MTT) assay. Apoptosis rate and cell cycle detection were performed by flow cytometry. Western blot was used to determine the protein kinase B (Akt), phosphorylated Akt (p-Akt) and cyclinD1. Result: The average particle size of the prepared Jug-PLGA-NPs was (149.6±21.5) nm, entrapment rate of (68.39±2.51)%, and drug-loading rate of (5.07±0.98)%, showing good sustained-release characteristics. PLGA-NPs showed good penetration and targeting properties in cellular uptake in vitro and in vivo imaging. Different concentrations of Jug-PLGA-NPs could significantly inhibit the proliferation and promote apoptosis of A375 cells in a time and concentration dependent manner (P<0.05), and its 48 h effect was superior to that of the same concentration of Jug. The mechanism may be related to the regulation of Akt phosphorylation level, down-regulation of cyclinD1 expression (P<0.05) and the cell-cycle arrest in G0/G1 phase (P<0.05). Conclusion: The Jug-PLGA-NPs are easy to prepare and have good sustained-release characteristics, tumor targeting and anti-tumor ability, providing a new pharmaceutical dosage form for the future clinical application of Jug.
