Formulation design and in vivo antimalarial evaluation of lipid-based drug delivery systems for oral delivery of β-arteether.

Abstract

β-Arteether, an effective artemisinin derivative, is used in the treatment of malaria but available only as an intramuscular injection. The objective of this work was to develop lipid-based formulations for oral administration of β-arteether. Self-emulsifying drug delivery systems (SEDDSs) of low cost and with accessible excipients (groundnut or sesame oil, Maisine 35-1, Tween 80 or Cremophor EL, and absolute ethanol) were formulated. In 250 ml of simulated gastric medium, 1g of these SEDDS solubilized the daily dose of β-arteether and formed lipid droplets of average size 80-250 nm. No toxicity against Caco-2 intestinal cells was observed. Using a mouse model, the efficacy of these arteether lipid formulations against Plasmodium berghei was evaluated. A daily dose of 24 mg/kg for 4 days led to complete cure for more than 45 days in 100% of treated mice and had an antimalarial efficacy comparable to that of an intramuscular oily solution of arteether and significantly higher than that of an oily solution of β-arteether given orally at the same dose. In conclusion, lipid-based drug delivery systems constitute a promising approach for the oral administration of β-arteether.

DOI: 10.1016/j.ejpb.2012.05.004

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@article{Memvanga2012FormulationDA, title={Formulation design and in vivo antimalarial evaluation of lipid-based drug delivery systems for oral delivery of β-arteether.}, author={Patrick B. Memvanga and V{\'e}ronique Pr{\'e}at}, journal={European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V}, year={2012}, volume={82 1}, pages={112-9} }