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NOT Open Access | Artemisinin-type drugs for the treatment of hematological malignancies

November 4, 2020 - 15:11 -- NOT Open Access
Mancuso RI, Foglio MA, Olalla Saad ST
Cancer Chemother Pharmacol. 2020 Nov 3

Qinghaosu, known as artemisinin (ARS), has been for over two millennia, one of the most common herbs prescribed in traditional Chinese medicine (TCM). ARS was developed as an antimalarial drug and currently belongs to the established standard treatments of malaria as a combination therapy worldwide. In addition to the antimalarial bioactivity of ARS, anticancer activities have been shown both in vitro and in vivo.

NOT Open Access | Characterization of solid lipid dispersions prepared by hot fusion containing a double-fixed dose combination of artemether and lumefantrine

August 4, 2020 - 14:57 -- NOT Open Access
Wilkins CA, du Plessis LH, Viljoen JM
Drug Dev Ind Pharm. 2020 Aug; 46(8):1289-1297

The World Health Organization has called for the development of novel drug delivery systems to combat malaria – the fourth most prevalent cause of death globally. The plausibility of utilizing hot fusion to prepare solid lipid dispersions containing the prescribed first-line, double-fixed dose combination (artemether and lumefantrine), proposed for inclusion in directly compressed lipid matrix tablets, was investigated.

NOT Open Access | A Chemically Stable Fluorescent Mimic of Dihydroartemisinin, Artemether, and Arteether with Conserved Bioactivity and Specificity Shows High Pharmacological Relevance to the Antimalarial Drugs

July 20, 2020 - 14:52 -- NOT Open Access
Sissoko A, Vásquez-Ocmín P, Duval R, et al.
ACS Infect Dis. 2020 Jul 10; 6(7):1532-1547

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin.

NOT Open Access | A chemically stable fluorescent mimic of dihydroartemisinin, artemether and arteether with conserved bioactivity and specificity shows high pharmacological relevance to the antimalarial drugs

April 13, 2020 - 14:01 -- NOT Open Access
Sissoko A, Vasquez-Ocmin P, Duval RA, et al.
ACS Infect Dis. 2020 Apr 8

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i. e., dihydroartemisinin, artemether, arteether and artemisone) were synthesized from dihydroartemisinin.

Development of a dissolution method for lumefantrine and artemether in immediate release fixed dose artemether/lumefantrine tablets

April 10, 2020 - 17:12 -- Open Access
Sileshi Belew, Sultan Suleman, Markos Duguma, Henok Teshome, Evelien Wynendaele, Luc Duchateau and Bart De Spiegeleer
Malaria Journal 2020 19:139, 7 April 2020

Dissolution of artemether (ART) and lumefantrine (LUM) active pharmaceutical ingredients (APIs) in fixed dose combination (FDC) ART/LUM tablets is one of the critical quality attributes. Thus, the verification of the release profile of ART and LUM from FDC ART/LUM tablets using a robust and discriminatory dissolution method is crucial. Therefore, the aim of this study was to develop and validate an appropriate dissolution method for quality control of FDC ART/LUM tablets.

NOT Open Access | 22 factorial design-based biocompatible microneedle arrays containing artemether co-loaded with lumefantrine nanoparticles for transepidermal delivery

February 25, 2020 - 16:15 -- NOT Open Access
Pawar S, Shende P
Biomed Microdevices. 2020 Feb 19;22(1):19

The present study was intended to enhance the permeation of artemether and lumefantrine by encapsulating in dissolvable microneedle arrays for extended action. Lumefantrine-nanoparticles were synthesized using chitosan mediated gelation and optimized by 22 factorial designs.

Not Open Access | A high-performance liquid chromatography–tandem mass spectrometry method for the determination of artemether and dihydroartemisinin in human plasma

July 3, 2014 - 17:09 -- NOT Open Access
M.J. Hilhorst, G. Hendriks, R. de Vries, V. Hillewaert, T. Verhaege, N.C. van de Merbel
Journal of Chromatography B, Volume 965, 15 August 2014, Pages 45-53

The method was successfully used for the analysis of pharmacokinetic samples originating from a drug–drug interaction study in which the antimalarial drugs artemether/lumefantrine were coadministrated etravirine or darunavir/ritonavir in healthy human immunodeficiency virus (HIV)-negative subjects.

Not Open Access | The survival times of malaria-infected mice are prolonged more by several new two-carbon-linked artemisinin-derived dimer carbamates than by the trioxane antimalarial drug artemether

February 26, 2014 - 16:28 -- NOT Open Access
Ryan C. Conyers, Jennifer R. Mazzone, Maxime A. Siegler, Abhai K. Tripathi, David J. Sullivan, Bryan T. Mott, Gary H. Posner
Bioorganic & Medicinal Chemistry Letters, Volume 24, Issue 5, 1 March 2014, Pages 1285-1289

This ACT chemotherapy result is of high medicinal significance because the antimalarial efficacy of the popular trioxane drug artemether (2) plus mefloquine under the same conditions was significantly lower (only 20 day average survival). 

Azadirachta indica ethanolic extract protects neurons from apoptosis and mitigates brain swelling in experimental cerebral malaria

September 4, 2013 - 11:24 -- Open Access
Bedri S, Khalil EA, Khalid SA, Alzohairy MA, Mohieldein A, Aldebasi YH, Seke Etet PF, Farahna M
Malaria Journal 2013, 12:298 (29 August 2013)

The present findings suggest that Azadirachta indica ethanolic extract has protective effects on neuronal populations in the inflamed central nervous system, and justify at least in part its use in African and Asian folk medicine and practices.

Not Open Access | Evaluation of novel lipid based formulation of β-Artemether and Lumefantrine in murine malaria model

September 3, 2013 - 17:17 -- NOT Open Access
Sushant Patil, Shital Suryavanshi, Sulabha Pathak, Shobhona Sharma, Vandana Patravale
International Journal of Pharmaceutics, Volume 455, Issues 1–2, 15 October 2013, Pages 229-234

The present investigation aims at formulating lipid based drug delivery system of β-Artemether and Lumefantrine and comparative pharmacological evaluation with innovator formulation.


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