Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment

Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment

Abstract Solidified reverse micellar technology and surface-modification are promising techniques for improving the biopharmaceutical properties of poorly water-soluble drugs such as artemether, a first-line antimalarial drug. Thus, the aim of this study was to develop and evaluate artemether-loaded...

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Main Authors: Franklin Chimaobi Kenechukwu, Kingsley Chinazam Ugwu, Chibuzor Stanley Offorbuike, Enyi Moses Ojukwu, Thaddeus Harrison Gugu, Reuben Ejike Eze, Chinazom Precious Agbo, Mumuni Audu Momoh, Anthony Ikechukwu Onah, Chinekwu Sherridan Nwagwu, Onyinyechi Lydia Ugorji, Emmanuel Chekwube Ossai, Calister Elochukwu Ugwu, Paul Achile Akpa, Adaeze Chidiebere Echezona, Samuel WisdomofGod Uzondu, Chimaobi Odinaka Ugorji, Wilfred Ikechukwu Ugwuoke, Teerapol Srichana, Anthony Amaechi Attama
Format: Article
Language:English
Published: BMC 2025-03-01
Series:BMC Chemistry
Subjects:
Solidified reverse micellar solution
Antimalarial activity
Chitosan
Solid lipid nanoparticles
Artemether
Plasmodium berghei
Online Access:https://doi.org/10.1186/s13065-025-01422-4
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Summary:Abstract Solidified reverse micellar technology and surface-modification are promising techniques for improving the biopharmaceutical properties of poorly water-soluble drugs such as artemether, a first-line antimalarial drug. Thus, the aim of this study was to develop and evaluate artemether-loaded chitosan-coated solid lipid nanoparticles (SLNs) based on solidified reverse micellar solution (SRMS) for improved oral malaria therapy. Artemether-loaded and unloaded SLNs were prepared from optimized SRMS (consisting of Phospholipon® 90G and Compritol® ATO 888 at 3:7 ratio) with or without chitosan by high-shear melt-homogenization, and thereafter characterized for physicochemical performance, stability, safety and antimalarial activity using Plasmodium berghei-infected mice. Results showed both smooth and irregular particles with a layer of polymer coating in chitosan-modified SLNs, increased drug amorphization as well as compatibility of the drug and excipients employed in the formulations. The optimized formulation was stable and nanomeric (size 292.90 ± 5.01 nm, polydispersity index 0.191 ± 0.09, and zeta-potential + 32.50 ± 1.58 mV) with good encapsulation efficiency (82.03%), demonstrated minimal toxicity on Caco-2 cells, exhibited controlled drug release compared with fast release of artemether suspension and gave significantly (p < 0.05) greater antimalarial activity than artemether suspension. Artemether-loaded chitosan-coated SRMS-based SLNs improved the antimalarial activity of the drug and can be pursued as a novel alternative for improved oral malaria treatment.
ISSN:2661-801X

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