青蒿琥酯
PLGA公司
药理学
伯氏疟原虫
毒性
乙醇酸
化学
细胞毒性
体外
乳酸
医学
生物化学
恶性疟原虫
生物
免疫学
有机化学
疟疾
细菌
遗传学
作者
Kabiru Dauda,Zulaikha Busari,Olajumoke A. Morenikeji,Funmilayo I. D. Afolayan,Oyetunde T. Oyeyemi,Jairam Meena,D. R. Sahu,Amulya K. Panda
出处
期刊:Journal of Zhejiang University-science B
[Springer Nature]
日期:2017-11-01
卷期号:18 (11): 977-985
被引量:16
标识
DOI:10.1631/jzus.b1600389
摘要
The aim of this study was to formulate polymer-based artesunate nanoparticles for malaria treatment.Artesunate was loaded with poly(D,L-lactic-co-glycolic acid) (PLGA) by solvent evaporation from an oil-in-water single emulsion. Nanoparticles were characterized by X-ray diffraction and differential scanning calorimetry analyses. In vivo antimalarial studies at 4 mg/kg were performed on Swiss male albino mice infected with Plasmodium berghei. Hematological and hepatic toxicity assays were performed. In vitro cytotoxicity of free and encapsulated artesunate (Art-PLGA) to cell line RAW 264.7 was determined at concentrations of 7.8-1000 µg/ml.The particle size of the formulated drug was (329.3±21.7) nm and the entrapment efficiency was (38.4±10.1)%. Art-PLGA nanoparticles showed higher parasite suppression (62.6%) compared to free artesunate (58.2%, P<0.05). Platelet counts were significantly higher in controls (305 000.00±148 492.40) than in mice treated with free artesunate (139 500.00±20 506.10) or Art-PLGA (163 500.00±3535.53) (P<0.05). There was no sign of hepatic toxicity following use of the tested drugs. The half maximal inhibitory concentration (IC50) of Art-PLGA (468.0 µg/ml) was significantly higher (P<0.05) than that of free artesunate (7.3 µg/ml) in the in vitro cytotoxicity assay.A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.
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