Abstract
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.
Highlights
IntroductionMalaria is a life-threatening tropical disease caused by Plasmodium parasites that are transmitted to people through the bites of infected female Anopheles mosquitoes [1,2,3]
Malaria is a life-threatening tropical disease caused by Plasmodium parasites that are transmitted to people through the bites of infected female Anopheles mosquitoes [1,2,3].According to World Malaria Report 2020, there were 229 million cases worldwide and more than 400,000 people died of malaria in 2019 [3]
2, this artemether-load zein nanoparticles prepared by modfrom study will facilitate the development of anwere innovative therapeutic option for severe malaria
Summary
Malaria is a life-threatening tropical disease caused by Plasmodium parasites that are transmitted to people through the bites of infected female Anopheles mosquitoes [1,2,3]. According to World Malaria Report 2020, there were 229 million cases worldwide and more than 400,000 people died of malaria in 2019 [3]. The management of malaria has been revolutionarily improved by the introduction of the artemisinin derivatives in the 1990s, a group of semisynthetic compounds produced from artemisinin (Figure 1a), a sesquiterpene lactone endoperoxide originally isolated from the traditional Chinese herb Artemisia annua [1,6]. As artemisinin derivatives are rapidly effective, safe and well tolerated, artemisinin-based combination treatments are recommended by the World Health Organization (WHO) as first-line therapies in all malaria endemic countries [1,7].
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