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      Smart nanocrystals of artemether: fabrication, characterization, and comparative in vitro and in vivo antimalarial evaluation

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          Abstract

          Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena ® DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145.0±2.3 µg/mL) and stabilizer solution (300.0±2.0 µg/mL). The physical stability studies conducted for 90 days demonstrated that nanocrystals stored at 2°C–8°C and 25°C were very stable compared to the samples stored at 40°C. The nanocrystals were also shown to be stable when processed at acidic pH (2.0). The solubility and dissolution rate of ARTM nanocrystals were significantly increased ( P<0.05) compared to those of its bulk powder form. The results of in vitro studies showed significant antimalarial effect ( P<0.05) against Plasmodium falciparum and Plasmodium vivax. The IC 50 (median lethal oral dose) value of ARTM nanocrystals was 28- and 54-fold lower than the IC 50 value of unprocessed drug and 13- and 21-fold lower than the IC 50 value of the marketed tablets, respectively. In addition, ARTM nanocrystals at the same dose (2 mg/kg) showed significantly ( P<0.05) higher reduction in percent parasitemia (89%) against P. vivax compared to the unprocessed (27%), marketed tablets (45%), and microsuspension (60%). The acute toxicity study demonstrated that the LD 50 value of ARTM nanocrystals is between 1,500 mg/kg and 2,000 mg/kg when given orally. This study demonstrated that the wet milling technology (Dena ® DM-100) can produce smart nanocrystals of ARTM with enhanced antimalarial activities.

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          Most cited references 65

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          Human malaria parasites in continuous culture.

          Plasmodium falciparum can now be maintained in continuous culture in human erythrocytes incubated at 38 degrees C in RPMI 1640 medium with human serum under an atmosphere with 7 percent carbon dioxide and low oxygen (1 or 5 percent). The original parasite material, derived from an infected Aotus trivirgatus monkey, was diluted more than 100 million times by the addition of human erythrocytes at 3- or 4-day intervals. The parasites continued to reproduce in their normal asexual cycle of approximately 48 hours but were no longer highly synchronous. The have remained infective to Aotus.
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            Qinghaosu (artemisinin): an antimalarial drug from China.

             D L Klayman (1985)
            The herb Artemisia annua has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria. In 1971, Chinese chemists isolated from the leafy portions of the plant the substance responsible for its reputed medicinal action. This compound, called qinghaosu (QHS, artemisinin), is a sesquiterpene lactone that bears a peroxide grouping and, unlike most other antimalarials, lacks a nitrogen-containing heterocyclic ring system. The compound has been used successfully in several thousand malaria patients in China, including those with both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Derivatives of QHS, such as dihydroqinghaosu, artemether, and the water-soluble sodium artesunate, appear to be more potent than QHS itself. Sodium artesunate acts rapidly in restoring to consciousness comatose patients with cerebral malaria. Thus QHS and its derivatives offer promise as a totally new class of antimalarials.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2016
                24 November 2016
                : 10
                : 3837-3850
                Affiliations
                [1 ]Department of Pharmacy, Sarhad University of Science & Information Technology, Peshawar
                [2 ]Department of Pharmacy, University of Malakand, Chakdara, Pakistan
                [3 ]Institute of Life Sciences Research, School of Pharmacy, University of Bradford, West Yorkshire
                [4 ]Department of Pharmacy, University of Swabi, KPK, Pakistan
                [5 ]SEDA Pharmaceutical Development Services, The BioHub at Alderley Park, Cheshire, UK
                [6 ]Faculty of Pharmacy, Department of Pharmaceutics, Universiti Teknologi MARA, Selangor, Malaysia
                [7 ]Faculty of Pharmacy & Alternative Medicine, The Islamia University of Bahawalpur Pakistan, Bahawalpur, Pakistan
                [8 ]Riyadh Community College, King Saud University, Riyadh, Saudi Arabia
                Author notes
                Correspondence: Shahzeb Khan, Department of Pharmacy, University of Malakand, Chakdara 23050, Pakistan, Tel +92 34 5949 2869, Email shahzeb_333@ 123456hotmail.com
                Article
                dddt-10-3837
                10.2147/DDDT.S114962
                5125812
                © 2016 Shah et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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                Original Research

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