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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
pharmacology, toxicology and pharmaceutics
Absorption of the novel artemisinin derivatives artemisone and artemiside: Potential application of Pheroid™ technology
International Journal of Pharmaceutics, Volume 414, No. 1-2, Year 2011
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Description
Artemisinins have low aqueous solubility that results in poor and erratic absorption upon oral administration. The poor solubility and erratic absorption usually translate to low bioavailability. Artemisinin-based monotherapy and combination therapies are essential for the management and treatment of uncomplicated as well as cerebral malaria. Artemisone and artemiside are novel artemisinin derivatives that have very good antimalarial activities. Pheroid™ technology is a patented drug delivery system which has the ability to entrap, transport and deliver pharmacologically active compounds. Pharmacokinetic models were constructed for artemisone and artemiside in Pheroid™ vesicle formulations. The compounds were administered at a dose of 50.0 mg/kg bodyweight to C57 BL/6 mice via an oral gavage tube and blood samples were collected by means of tail-bleeding. Drug concentrations in the samples were determined using an LC/MS/MS method. There was 4.57 times more artemisone in the blood when the drug was entrapped in Pheroid™ vesicles in comparison to the drug only formulation (p < 0.0001). The absorption of artemiside was not dramatically enhanced by the Pheroid™ delivery system. © 2011 Elsevier B.V.
Authors & Co-Authors
Steyn, Dewald
South Africa, Potchefstroom
North-west University
Wiesner, L. D.
South Africa, Cape Town
Faculty of Health Sciences
Du Plessis, Lissinda Hester
South Africa, Potchefstroom
North-west University
Grobler, Anne F.
South Africa, Potchefstroom
North-west University
Smith, Peter John
South Africa, Cape Town
Faculty of Health Sciences
Chan, Wing Chi
Hong Kong, Hong Kong
Hong Kong University of Science and Technology
Haynes, Richard K.
Hong Kong, Hong Kong
Hong Kong University of Science and Technology
Kotzé, Awie F.
South Africa, Potchefstroom
North-west University
Statistics
Citations: 50
Authors: 8
Affiliations: 3
Identifiers
Doi:
10.1016/j.ijpharm.2011.05.003
ISSN:
03785173
e-ISSN:
18733476
Research Areas
Health System And Policy
Infectious Diseases