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NOT Open Access | Formulation development and characterization of Lumefantrine nanosuspension for enhanced antimalarial activity

January 6, 2021 - 12:59 -- NOT Open Access
Shah R, Soni T, Shah U, Suhagia BN, Patel MN, Patel T, Gabr GA, Gorain B, Kesharwani P
J Biomater Sci Polym Ed. 2020 Dec 30:1-18

Variable and low oral bioavailability (4-11%) of lumefantrine (LUF), an anti-malarial agent, is characterized by very low solubility in aqueous vehicle. Thus, the present study was intended to formulate lyophilized nanosuspensions of LUF to resolve its solubility issues for the improvement of oral bioavailability. A three level 32 factorial design was applied to analyze the influence of independent variables, concentration of polysorbate 80 (X1) and sonication time (X2) on the responses for dependent variables, particle size (Y1) and time to 90% release of LUF (t90) (Y2).

Tolerance of Gambian Plasmodium falciparum to Dihydroartemisinin and Lumefantrine detected by Ex vivo Parasite Survival Rate Assay (PSRA)

October 7, 2020 - 15:39 -- Open Access
Mbye H, Bojang F, Jawara AS, Njie B, Mohammed NI, Okebe J, D'Alessandro U, Amambua-Ngwa A
Antimicrob Agents Chemother. 2020 Oct 5:AAC.00720-20

Monitoring of Plasmodium falciparum sensitivity to antimalarial drugs in Africa is vital for malaria elimination. However, the commonly used ex-vivo/in-vitro IC50 test is inconsistent for several antimalarials, while the alternative ring-stage survival assay (RSA) for artemisinin derivatives has not been widely adopted. Here we applied an alternative two-colour flow-cytometry based parasite survival rate assay (PSRA) to detect ex-vivo antimalarial tolerance in P. falciparum isolates from The Gambia.

Antimalarial drugs inhibit the replication of SARS-CoV-2: an in vitro evaluation

September 15, 2020 - 14:26 -- Open Access
Gendrot M, Andreani J, Pradines B, et al.
Travel Med Infect Dis. 2020 Sep 8:101873

In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2) causing coronavirus diseases 2019 (COVID-19) emerged in Wuhan, China. African countries see slower dynamic of COVID-19 cases and deaths. One of the assumptions that may explain this later emergence in Africa, and more particularly in malaria endemic areas, would be the use of antimalarial drugs.

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.

Plasmodium falciparum genetic factors rather than host factors are likely to drive resistance to ACT in Ghana

July 20, 2020 - 14:50 -- Open Access
Peter Hodoameda, Nancy Odurowah Duah-Quashie, Charles Oheneba Hagan, Sena Matrevi, Benjamin Abuaku, Kwadwo Koram and Neils Ben Quashie
Malaria Journal 2020 19:255, 15 July 2020

Artemisinin-based combination therapy (ACT) partner drugs, currently used in Ghana are lumefantrine, amodiaquine and piperaquine. Plasmodium falciparum isolates with reduced susceptibility to these partner drugs may affect treatment outcome. Mutations in pfmdr1 gene is linked to reduced parasite susceptibility to amodiaquine and lumefantrine. In addition, the potency of the partner drugs in vivo depends on the metabolism by the cytochrome P450 (CYP) enzyme in the host. Mutations in the CYP2C8 and CYP3A4 genes are linked to reduced metabolism of amodiaquine and lumefantrine in vitro, respectively. This study investigated the host and parasite genetic factors affecting the susceptibility of the malaria parasite to ACT partner drugs.

NOT Open Access | Evidence of Microbiome-Drug Interactions between the Antimalarial Lumefantrine and Gut Microbiota in Mice

July 7, 2020 - 13:02 -- NOT Open Access
Ippolito MM, Denny JE, Nenortas E, Shapiro TA, Schmidt NW
Am J Trop Med Hyg. 2020 Jul 6

The antimalarial drug lumefantrine (LF) exhibits erratic pharmacokinetics (PK). Intersubject variability might be attributed, in part, to differences in the gut microbiome-mediated drug metabolism. We assessed LF disposition in healthy mice stratified by enterotype to explore associations between the gut microbiota and LF PK. Gut microbiota enterotypes were classified according to abundance and diversity indices from 16S rRNA sequencing.

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.

Drug-drug Interactions between Lumefantrine and Commonly-used Antiretroviral Treatment: An Individual Participant Data Population Pharmacokinetic Meta-Analysis

February 24, 2020 - 14:10 -- Open Access
Francis J, Barnes KI, Denti P, et al.
Antimicrob Agents Chemother. 2020 Feb 18. pii: AAC.02394-19

Treating malaria in HIV co-infected individuals should consider potential drug-drug interactions. Artemether-lumefantrine is the most widely recommended treatment for uncomplicated malaria globally. Lumefantrine is metabolized by CYP3A4, an enzyme that commonly-used antiretrovirals often induce or inhibit. A population pharmacokinetic meta-analysis was conducted using individual participant data from ten studies, with 6,100 lumefantrine concentrations from 793 non-pregnant adult participants (41% HIV-malaria co-infected, 36% malaria-infected, 20% HIV-infected, and 3% healthy volunteers).

Plasmodium falciparum susceptibility to standard and potential anti-malarial drugs in Dakar, Senegal, during the 2013–2014 malaria season

March 4, 2015 - 15:06 -- Open Access
Bécaye Fall, Cheikhou Camara, Mansour Fall, Aminata Nakoulima, Pierre Dionne, Bakary Diatta, Yaya Diemé, Boubacar Wade, Bruno Pradines
Malaria Journal 2015, 14:60 (6 February 2015)

The prevalence of isolates with a reduced susceptibility to MQ remains high and stable in Dakar. Since 2004, the prevalence of CQ resistance decreased, but rebounded in 2013 in Dakar. PND, PPQ and PVB showed high in vitro activity in P. falciparum parasites from Dakar


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