Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria
1
Institute of Chemical and Engineering Sciences, Agency for Science, Technology and Research, 1 Pesek Road, Jurong Island, Singapore 627833, Singapore
2
Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
3
Department of Pharmaceutical Sciences, Sunyani Technical University, P.O. Box 206 Sunyani, Ghana
4
College of Pharmacy, Shenzhen Technology University, 3002 Lantian Road, Pingshan District, Shenzhen 518118, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Maciej Jarzębski
Int. J. Mol. Sci. 2021, 22(3), 1141; https://doi.org/10.3390/ijms22031141
Received: 4 January 2021 / Revised: 16 January 2021 / Accepted: 17 January 2021 / Published: 24 January 2021
(This article belongs to the Special Issue Multidisciplinary Investigations of Nanoparticle Synthesis and Analysis for Possible Biomedical and Food Technology Applications)
Artemether, an artemisinin derivative, is used in the management of life-threatening severe malaria. This study aimed to develop an intravenous dosage form of artemether using nanotechnology. Artemether-loaded zein nanoparticles were prepared by modified antisolvent precipitation using sodium caseinate as a stabilizer. Subsequently, the physicochemical properties of the nanoparticles were characterized; the in vitro hemolytic property was examined with red blood cells, while the pharmacokinetic profile was evaluated in Sprague–Dawley rats after intravenous administration. The artemether-loaded zein nanoparticles were found to display good encapsulation efficiency, excellent physical stability and offer an in vitro extended-release property. Interestingly, encapsulation of artemether into zein nanoparticles substantially suppressed hemolysis, a common clinical phenomenon occurring after artemisinin-based antimalarial therapy. Upon intravenous administration, artemether-loaded zein nanoparticles extended the mean residence time of artemether by ~80% in comparison to the free artemether formulation (82.9 ± 15.2 versus 45.6 ± 16.4 min, p < 0.01), suggesting that the nanoparticles may prolong the therapeutic duration and reduce the dosing frequency in a clinical setting. In conclusion, intravenous delivery of artemether by artemether-loaded zein nanoparticles appears to be a promising therapeutic option for severe malaria.
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Keywords:
artemether; artemisinin; extended release; hemolysis; intravenous; nanoparticles; pharmacokinetics; severe malaria; sodium caseinate; zein
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MDPI and ACS Style
Boateng-Marfo, Y.; Dong, Y.; Ng, W.K.; Lin, H.-S. Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria. Int. J. Mol. Sci. 2021, 22, 1141. https://doi.org/10.3390/ijms22031141
AMA Style
Boateng-Marfo Y, Dong Y, Ng WK, Lin H-S. Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria. International Journal of Molecular Sciences. 2021; 22(3):1141. https://doi.org/10.3390/ijms22031141
Chicago/Turabian StyleBoateng-Marfo, Yaa; Dong, Yuancai; Ng, Wai K.; Lin, Hai-Shu. 2021. "Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria" Int. J. Mol. Sci. 22, no. 3: 1141. https://doi.org/10.3390/ijms22031141
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