NANOPARTICLE-BASED formulation of dihydroartemisinin-lumefantrine duo-drugs: Preclinical Evaluation and enhanced antimalarial efficacy in a mouse model.

Autor:	Odera PA; School of Chemistry and Material Science, Technical University of Kenya, Nairobi Kenya., Otieno G; School of Chemistry and Material Science, Technical University of Kenya, Nairobi Kenya., Onyango JO; School of Chemistry and Material Science, Technical University of Kenya, Nairobi Kenya., Owuor JJ; School of Chemistry and Material Science, Technical University of Kenya, Nairobi Kenya., Oloo FA; School of Chemistry and Material Science, Technical University of Kenya, Nairobi Kenya.; Centre for Research in Therapeutic Sciences, Strathmore University Medical Centre, Nairobi, Kenya., Ongas M; Centre for Clinical Research, Kenya Medical Research Institute, Nairobi, Kenya.; Centre for Research in Therapeutic Sciences, Strathmore University Medical Centre, Nairobi, Kenya., Gathirwa J; Centre of Traditional Medicine and Drug Research, Kenya Medical Research Institute, Nairobi, Kenya., Ogutu B; Centre for Clinical Research, Kenya Medical Research Institute, Nairobi, Kenya.; Centre for Research in Therapeutic Sciences, Strathmore University Medical Centre, Nairobi, Kenya.
Jazyk:	angličtina
Zdroj:	Heliyon [Heliyon] 2024 Feb 23; Vol. 10 (6), pp. e26868. Date of Electronic Publication: 2024 Feb 23 (Print Publication: 2024).
DOI:	10.1016/j.heliyon.2024.e26868
Abstrakt:	Artemisinin-based combinations (ACTs) are World Health Organization-recommended treatment for malaria. Artemether (A) and lumefantrine (LUM) were the first co-formulated ACT and first-line treatment for malaria globally, artemether is dihydroartemisinin's (DHA's) prodrug. Artemisinins and LUM face low aqueous solubility while artemisinin has low bioavailability and short half-life thus requiring continuous dosage to maintain adequate therapeutic drug-plasma concentration. This study aimed at improving ACTs limitations by nano-formulating DHA-LUM using solid lipid nanoparticles (SLNs) as nanocarrier. SLNs were prepared by modified solvent extraction method based on water-in-oil-in-water double emulsion. Mean particle size, polydispersity index and zeta potential were 308.4 nm, 0.29 and -16.0 mV respectively. Nanoencapsulation efficiencies and drug loading of DHA and LUM were 93.9%, 33.7%, 11.9%, and 24.10% respectively. Nanoparticles were spherically shaped and drugs followed Kors-Peppas release model, steadily released for over 72 h. DHA-LUM-SLNs were 31% more efficacious than conventional oral doses in clearing Plasmodium berghei from infected Swiss albino mice. Competing Interests: The authors declare the following financial interests/personal relationships which may be considered as potential competing interests:Dr. Bernards Ogutu reports financial support, administrative support, equipment, drugs, or supplies, statistical analysis, and travel were provided by the National Research Fund, Kenya. NONE has a patent NONE pending to NONE. NONE If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (© 2024 The Authors.)
Databáze:	MEDLINE
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