Solid lipid nanoparticles encapsulating a fluorescent marker (coumarin 6) and antimalarials – artemether and lumefantrine: evaluation of cellular uptake and antimalarial activity

Attama, Anthony A.; Kenechukwu, Franklin Chimaobi; Onuigbo, Ebele; Nnamani, Petra O.; Obitte, Nicholas C.; Finke, Jan Henrik; Pretor, Sascha; Müller‐Goymann, Christel C.

doi:10.1515/nano.0012.2016-0009

Cited by 6 publications

(12 citation statements)

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“…The values of the parameters reduced post inoculation with the parasite on day 3, but showed a progressive stabilized increase on day 7 post-treatment. This efficacy was observed in other murine models, as described by Attama et al 27 .…”

Section: Discussionsupporting

confidence: 73%

Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution

Echezona

Momoh

Akpa

et al. 2020

J. Drug Delivery Ther.

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Malaria, a leading cause of mortality and morbidity in the developing world, with children aged under 5 years, accounts for 61% of all the global malaria deaths. The World Health Organization approved fixed-dose first-line artemisinin-based combination therapy (ACT) – artemether-lumefantrine for effective malaria treatment, is challenged by poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains. This study focuses on evaluating novel lumefantrine (LF) polymethacrylate-urea solid solutions comprising of a retarding polymer for enhanced anti-plasmodial efficacy comparable with existing artemether-lumefantrine combination therapy. Lumefantrine polymethacrylate-urea solid solutions were prepared by solvent evaporation and characterized by differential scanning calorimetry (DSC), and dissolution studies. In vivo anti-plasmodial activity was determined by measuring the schizonticidal activity of Plasmodium berghei-infected mice using the Peter’s 4-day curative test and the safety of the solid solutions was tested in major organs implicated in malaria. The solid state characterizations confirmed the formation of amorphous lumefantrine polymethacrylate-urea solid solutions. There was greater drug release from the matrix polymer in acidic than basic biorelevant media, with release kinetics following the Higuchi order. Interestingly, the reduction in parasitaemia caused by the lumefantrine polymethacrylate-urea formulations (72.3 and 81.27 %) for ternary and quaternary systems, batches SDA3 and SDB3, respectively) were significantly higher (p < 0.05) and more sustained than lumefantrine pure powder, but with comparable efficacy to the commercial brand-Coartem®. The formulation was stable over a period of 6 months. Thus, this study provides useful information on developing sustained lumefantrine formulation with improved solubility and antiplasmodial efficacy. Keywords: Solid dispersion, lumefantrine, solubility, parasitaemia reduction, eudragit polymer, Urea.

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Section: Discussionsupporting

confidence: 73%

Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution

Echezona

Momoh

Akpa

et al. 2020

J. Drug Delivery Ther.

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“…During crystallization, the material goes through different stages beginning with nucleation and followed by unhindered growth and structure formation. The initial nucleation is characterized by the appearance of nuclei far apart from each other leading to nonuniform crystallization, which may result in mixture of crystals and low crystal order capable of increasing drug loading capacity of the material [ 39 ]. The solubility limit of miconazole nitrate in the lipid matrices (PEGylated and non-PEGylated) was determined to be 3.0 %w/w.…”

Section: Resultsmentioning

confidence: 99%

“…The rate of crystallization of the drug would affect the ultimate size of the microparticle. If the drug crystallizes faster than the lipid matrix (as was the case with 5.0 % MN), encapsulation efficiency is expected to be higher and vice versa [ 39 ]. Further details of the results of the static crystallization could be found in the supplementary file 3 (Fig.…”

Section: Resultsmentioning

confidence: 99%

“…Drug-lipid matrix compatibility study performed by polarized light microscopy (PLM) was done to screen the drug and the excipients for solubility determination [ 39 ]. Each selected lipid matrix was melted by fusion in paraffin oil bath at 80°C using a thermoregulated hot plate, after weighing appropriate amount and different concentrations (0.5, 1.0, 2.0, 3.0, and 5.0 %w/w) of MN in 10.0 %w/w of each selected lipid matrix were weighed in an analytical balance and added to the melted lipid, followed by stirring using a magnetic stirrer-hot plate assembly at 100 rpm for 10 min.…”

Section: Methodsmentioning

confidence: 99%

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Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

Kenechukwu

Attama

Ibezim

et al. 2018

BioMed Research International

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The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan® 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability. Spherical discrete microparticles with good physicochemical properties and mean diameters suitable for vaginal drug delivery were obtained. Formulations based on SO:SF (1:9) and containing highest concentrations of PEG-4000 (4 %w/w) and MN (3.0 %w/w) were stable and gave highest encapsulation efficiency (83.05–87.75%) and inhibition zone diameter (25.87±0.94–26.33±0.94 mm) and significantly (p<0.05) faster and more powerful fungicidal activity regarding killing rate constant values (7.10 x 10−3–1.09 x 10−2 min−1) than commercial topical solution of MN (Fungusol®) (8.00 x 10−3 min−1) and pure MN sample (5.160 x 10−3 min−1). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC.

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“…In vitro studies using Caco-2 cells showed the ability of the lipid nanoparticles to deliver the drug to the gastrointestinal tract. In vivo studies indicated a high clearance of parasitemia with minimal side effects [ 166 ].…”

Section: Nanoparticlesmentioning

confidence: 99%

Nanoparticles Formulations of Artemisinin and Derivatives as Potential Therapeutics for the Treatment of Cancer, Leishmaniasis and Malaria

Alven

Aderibigbe

2020

Pharmaceutics

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Cancer, malaria, and leishmaniasis remain the deadly diseases around the world although several strategies of treatment have been developed. However, most of the drugs used to treat the aforementioned diseases suffer from several pharmacological limitations such as poor pharmacokinetics, toxicity, drug resistance, poor bioavailability and water solubility. Artemisinin and its derivatives are antimalarial drugs. However, they also exhibit anticancer and antileishmanial activity. They have been evaluated as potential anticancer and antileishmanial drugs but their use is also limited by their poor water solubility and poor bioavailability. To overcome the aforementioned limitations associated with artemisinin and its derivatives used for the treatment of these diseases, they have been incorporated into nanoparticles. Several researchers incorporated this class of drugs into nanoparticles resulting in enhanced therapeutic outcomes. Their potential efficacy for the treatment of parasitic infections such as malaria and leishmaniasis and chronic diseases such as cancer has been reported. This review article will be focused on the nanoparticles formulations of artemisinin and derivatives for the treatment of cancer, malaria, and leishmaniasis and the biological outcomes (in vitro and in vivo).

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Solid lipid nanoparticles encapsulating a fluorescent marker (coumarin 6) and antimalarials – artemether and lumefantrine: evaluation of cellular uptake and antimalarial activity

Cited by 6 publications

References 0 publications

Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution

Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution

Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

Nanoparticles Formulations of Artemisinin and Derivatives as Potential Therapeutics for the Treatment of Cancer, Leishmaniasis and Malaria

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