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 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. RESULTS: 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. CONCLUSIONS: A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.
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 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. RESULTS: 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. CONCLUSIONS: A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.
Authors: L Tona; K Mesia; N P Ngimbi; B Chrimwami; K Cimanga; T de Bruyne; S Apers; N Hermans; J Totte; L Pieters; A J Vlietinck Journal: Ann Trop Med Parasitol Date: 2001-01
Authors: Stefanie Wohlfart; Alexander S Khalansky; Svetlana Gelperina; Olga Maksimenko; Christian Bernreuther; Markus Glatzel; Jörg Kreuter Journal: PLoS One Date: 2011-05-06 Impact factor: 3.240
Authors: Luana Roberta Michels; Tamara Ramos Maciel; Kelly Ayumi Nakama; Flavia Elizabete Guerra Teixeira; Felipe Barbosa de Carvalho; André Gundel; Bibiana Verlindo de Araujo; Sandra Elisa Haas Journal: Int J Nanomedicine Date: 2019-12-31
Authors: Loick P Kojom Foko; Francois Eya'ane Meva; Carole E Eboumbou Moukoko; Agnes A Ntoumba; Marie I Ngaha Njila; Philippe Belle Ebanda Kedi; Lawrence Ayong; Leopold G Lehman Journal: Malar J Date: 2019-10-03 Impact factor: 2.979