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Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology

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dc.contributor.author Grobler, Anne Frederica
dc.contributor.author Smith, Peter
dc.contributor.author Steyn, Johan Dewald
dc.contributor.author Wiesner, Lubbe
dc.contributor.author Du Plessis, Lissinda Hester
dc.contributor.author Smith, Peter J.
dc.contributor.author Chan, Wing-Chi
dc.contributor.author Haynes, Richard K.
dc.contributor.author Kotzé, Abraham Frederick (Awie
dc.date.accessioned 2012-10-19T13:14:44Z
dc.date.available 2012-10-19T13:14:44Z
dc.date.issued 2011
dc.identifier.citation Steyn, J.D. et al. 2011. Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology. International Journal Of Pharmaceutics, 414(1-2):260-266. [http://www.journals.elsevier.com/international-journal-of-pharmaceutics/] en_US
dc.identifier.issn 0378-5173
dc.identifier.issn 1873-3476 (Online)
dc.identifier.uri http://hdl.handle.net/10394/7531
dc.description.abstract 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. en_US
dc.description.uri http://dx.doi.org/10.1016/j.ijpharm.2011.05.003
dc.language.iso en en_US
dc.publisher Elsevier en_US
dc.subject Malaria en_US
dc.subject artemisone en_US
dc.subject artemiside en_US
dc.subject Pheroid™ technology en_US
dc.subject pharmacokinetic analysis en_US
dc.title Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology en_US
dc.type Article en_US


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