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Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether

August 4, 2021 - 16:26 -- Open Access
Daniel J Watson, Lizahn Laing, Liezl Gibhard, Ho Ning Wong, Richard K Haynes, Lubbe Wiesner
Antimicrob Agents Chemother. 2021 Jul 16;65(8):e0099021

As artemisinin combination therapies (ACTs) are compromised by resistance, we are evaluating triple combination therapies (TACTs) comprising an amino-artemisinin, a redox drug, and a third drug with a different mode of action. Thus, here we briefly review efficacy data on artemisone, artemiside, other amino-artemisinins, and 11-aza-artemisinin and conduct absorption, distribution, and metabolism and excretion (ADME) profiling in vitro and pharmacokinetic (PK) profiling in vivo via intravenous (i.v.) and oral (p.o.) administration to mice.

NOT Open Access | The pharmacokinetic properties of artemether and lumefantrine in Malaysian patients with Plasmodium knowlesi malaria

July 28, 2021 - 14:05 -- NOT Open Access
Sugiarto SR, Singh B, Page-Sharp M, Davis WA, Salman S, Hii KC, Davis TME
Br J Clin Pharmacol. 2021 Jul 23

To assess the pharmacokinetic properties of artemether, lumefantrine and their active metabolites in Plasmodium knowlesi malaria.

Whole blood transfusion improves vascular integrity and increases survival in artemether-treated experimental cerebral malaria

June 15, 2021 - 14:27 -- Open Access
Gul S, Ribeiro-Gomes FL, Moreira AS, Sanches GS, Conceição FG, Daniel-Ribeiro CT, Ackerman HC, Carvalho LJM
Sci Rep. 2021 Jun 8;11(1):12077

Pathological features observed in both human and experimental cerebral malaria (ECM) are endothelial dysfunction and changes in blood components. Blood transfusion has been routinely used in patients with severe malarial anemia and can also benefit comatose and acidotic malaria patients. In the present study Plasmodium berghei-infected mice were transfused intraperitoneally with 200 μL of whole blood along with 20 mg/kg of artemether.

NOT Open Access | Artemether and lumefantrine dissolving microneedle patches with improved pharmacokinetic performance and antimalarial efficacy in mice infected with Plasmodium yoelii

May 19, 2021 - 15:26 -- NOT Open Access
Volpe-Zanutto F, Ferreira LT, Foglio MA, et al.
J Control Release. 2021 May 10;333:298-315

Malaria affects more than 200 million people annually around the world, killing a child every 2 min. Artemether (ART) and lumefantrine (LUM) are the gold standard choice to treat uncomplicated Plasmodium falciparum malaria; however, they are hydrophobic compounds with low oral bioavailability. Microneedle (MN) arrays consist of micron-sized needles on one side of a supporting base and have the ability to bypass the skin's stratum corneum barrier in a minimally invasive way, creating temporary channels through which drugs can diffuse, including those with poor water solubility.

NOT Open Access | Formulation and evaluation of transdermal nanogel for delivery of artemether

March 24, 2021 - 14:01 -- NOT Open Access
Nnamani PO, Ugwu AA, Nnadi OH, Kenechukwu FC, Ofokansi KC, Attama AA, Lehr CM
Drug Deliv Transl Res. 2021 Mar 19

Artemether (ART) is second to artesunate in being the most widely used derivatives of artemisinin in combination therapy of malaria. Nanostructured lipid carrier (NLC) formulations were prepared following our previous report using optimized ART concentration of 0.25 g dissolved in 5% w/v mixture of solid (Gelucire 43/01 and Phospholipon 85G) and liquid (Transcutol) lipids at 90 °C. An aqueous surfactant phase at 90 °C was added (dropwise) under magnetic stirring (1000 rpm) for 5 min. The pre-emulsion was speedily homogenized at 28,000 rpm for 15 min and further probe sonicated at 60% amplitude (15 min). Resultant sample was cooled at room temperature and frozen at - 80 °C prior to lyophilization.

NOT Open Access | Choline and PEG dually modified artemether nano delivery system targeting intra-erythrocytic Plasmodium and its pharmacodynamics in vivo

March 2, 2021 - 15:17 -- NOT Open Access
Wang R, Shi G, Chai L, Wang R, Zhang G, Ren G, Zhang S
Drug Dev Ind Pharm. 2021 Mar 1:1-11

The choline derivative (CD) and polyethylene-glycol (PEG) dually modified artemether (ARM) nanostructured lipid carriers (CD-PEG-ARM-NLC) have been designed to prolong the circulation of ARM in blood, as well as to develop targeting for new permeability pathways (NPPs) and erythrocyte choline carriers (ECCs) that are expressed on the Plasmodium-infected erythrocyte membrane.

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.


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