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Formulation design and in vivo antimalarial evaluation of lipid-based drug delivery systems for oral delivery of β-arteether
- Source :
-
European Journal of Pharmaceutics & Biopharmaceutics . Sep2012, Vol. 82 Issue 1, p112-119. 8p. - Publication Year :
- 2012
-
Abstract
- 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 250ml of simulated gastric medium, 1g of these SEDDS solubilized the daily dose of β-arteether and formed lipid droplets of average size 80–250nm. 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 24mg/kg for 4days led to complete cure for more than 45days 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. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 09396411
- Volume :
- 82
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- European Journal of Pharmaceutics & Biopharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 79805074
- Full Text :
- https://doi.org/10.1016/j.ejpb.2012.05.004