Issue 59, 2020

Potent in vivo antimalarial activity of water-soluble artemisinin nano-preparations

Abstract

Artemisinin is a remarkable compound whose derivatives and combinations with multiple drugs have been utilized at the forefront of malaria treatment. However, the inherent issues of the parent compound such as poor bioavailability, short serum half-life, and high first-pass metabolism partially limit further applications of this drug. In this study, we enhanced the aqueous phase solubility of artemisinin by encapsulating it in two nanocarriers based on the polymer polycaprolactone (ART-PCL) and lipid-based Large Unilamellar Vesicles (ART-LIPO) respectively. Both nanoformulations exhibit in vitro parasite killing activity against Plasmodium falciparum with the ART-LIPO performing at comparable efficacy to the control drug solubilized in ethanol. These water-soluble formulations showed potent in vivo antimalarial activity as well in the mouse model of malaria at equivalent doses of the parent drug. Additionally, the artemisinin-PCL nanoformulation used in combination with either pyrimethamine or chloroquine increased the survival of the Plasmodium berghei infected mice for more than 34 days and effectively cured the mice of the infection. We highlight the potential for polymer and liposome-based nanocarriers in improving not only the aqueous phase solubility of artemisinin but also concomitantly retaining its therapeutic efficacy in vivo as well.

Graphical abstract: Potent in vivo antimalarial activity of water-soluble artemisinin nano-preparations

Supplementary files

Article information

Article type
Paper
Submitted
26 Jun 2020
Accepted
22 Sep 2020
First published
01 Oct 2020
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2020,10, 36201-36211

Potent in vivo antimalarial activity of water-soluble artemisinin nano-preparations

P. Valissery, R. Thapa, J. Singh, D. Gaur, J. Bhattacharya, A. P. Singh and S. K. Dhar, RSC Adv., 2020, 10, 36201 DOI: 10.1039/D0RA05597B

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