Objective： The aim of this study was to formulate polymer-based artesunate nanoparticles for malaria treatment. Methods： Artesunate was loaded with poly（D,L-lactic-co-glycolic acid） （PLGA） by solvent evaporation...Objective： The aim of this study was to formulate polymer-based artesunate nanoparticles for malaria treatment. Methods： 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 calo- rimetry 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 en- capsulated artesunate （Art-PLGA） to cell line RAW 264.7 was determined at concentrations of 7.8-1000 pg/ml. Re- sults： 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 pg/ml） was significantly higher （P〈0.05） than that of free artesunate （7.3 pg/ml） in the in vitro cytotoxicity assay. Conclusions： A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.展开更多
In the 1970 s, artemisinin(‘‘qinghaosu'' in Chinese), a sesquiterpene lactone with an unusual peroxide bridge, was isolated from Artemisia annua L. It showed promising antimalarial activity, particularly by ...In the 1970 s, artemisinin(‘‘qinghaosu'' in Chinese), a sesquiterpene lactone with an unusual peroxide bridge, was isolated from Artemisia annua L. It showed promising antimalarial activity, particularly by eliminating parasites resistant to chloroquine. For more than 30 years,artemisinin has contributed to worldwide health as a new type of antimalarial drug. Artemisinin and its analogs, such as dihydroartemisinin, artemether, artesunate, artemiside,artemisone, and arteether, possess not only potent antimalarial activity but also anti-viral, antifungal, anticancer,and anti-inflammatory properties. In this review, we discuss the current understanding of how artemisinin and its analogs affect the immune system and immune-related diseases.展开更多
文摘Objective： The aim of this study was to formulate polymer-based artesunate nanoparticles for malaria treatment. Methods： 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 calo- rimetry 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 en- capsulated artesunate （Art-PLGA） to cell line RAW 264.7 was determined at concentrations of 7.8-1000 pg/ml. Re- sults： 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 pg/ml） was significantly higher （P〈0.05） than that of free artesunate （7.3 pg/ml） in the in vitro cytotoxicity assay. Conclusions： A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.
基金supported by the National Natural Science Foundation of China (91529305, 81427805, 81302507, 81302809, 31401611, 81573161, and 81502122)the Ministry of Science and Technology of China (2014AA020524)+2 种基金the CAS/ SAFEA International Partnership Program for Creative Research Teams of the Chinese Academy of Sciencesthe Science and Technology Commission of Shanghai Municipality (14391901800)the Key Laboratory of Food Safety Research of INS, SIBS, CAS
文摘In the 1970 s, artemisinin(‘‘qinghaosu'' in Chinese), a sesquiterpene lactone with an unusual peroxide bridge, was isolated from Artemisia annua L. It showed promising antimalarial activity, particularly by eliminating parasites resistant to chloroquine. For more than 30 years,artemisinin has contributed to worldwide health as a new type of antimalarial drug. Artemisinin and its analogs, such as dihydroartemisinin, artemether, artesunate, artemiside,artemisone, and arteether, possess not only potent antimalarial activity but also anti-viral, antifungal, anticancer,and anti-inflammatory properties. In this review, we discuss the current understanding of how artemisinin and its analogs affect the immune system and immune-related diseases.
