Journal
JOURNAL OF CONTROLLED RELEASE
Volume 172, Issue 3, Pages 904-913Publisher
ELSEVIER
DOI: 10.1016/j.jconrel.2013.09.001
Keywords
Curcumin; beta-arteether; Lipid-based formulations; Oral delivery; Caco-2 cells; Antimalarial efficacy
Funding
- Universite Catholique de Louvain (Bourse de la cooperation au developpement)
- scholarship of Patrick Bondo Memvanga
Ask authors/readers for more resources
Curcumin (CC), a potential antimalarial drug, has poor water solubility, stability and oral bioavailability. To circumvent these pitfalls, lipid-based drug delivery systems (LBDDSs) with a high CC loading (30 mg/g) were formulated. In a biorelevant gastric medium, CC-LBDDSs formed particle sizes in the range of 30-40 nm. During in vitro lipolysis, 90-95% of the CC remained solubilized, whereas 5-10% of the CC precipitated as an amorphous solid, with a high rate of re-dissolution in a biorelevant intestinal medium. The transport of the CC-LBDDS across Caco-2 monolayers was enhanced compared with the transport of free drug because of the increased CC solubility. In Plasmodium berghei-infected mice, modest antimalarial efficacy was observed following oral treatment with CC-LBDDSs. However, the combination therapy of CC-LBDDS with a subtherapeutic dose of beta-arteether-LBDDS provided an increase in protection and survival rate that was associated with a significant delay in recrudescence. These findings suggest that the combination of oral CC and beta-arteether lipid-based formulations may constitute a promising approach for the treatment of malaria. (C) 2013 Elsevier B.V. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available