African Health Sciences
Makerere University Medical School
Vol. 20, No. 4, 2020, pp. 1679-1697
Bioline Code: hs20124
Full paper language: English
Document type: Research Article
Document available free of charge
African Health Sciences, Vol. 20, No. 4, 2020, pp. 1679-1697
© Copyright 2020 - Akpa PA et al.
Improved antimalarial activity of caprol-based nanostructured lipid carriers encapsulating artemether-lumefantrine for oral administration|
Akpa, Paul Achile; Ugwuoke, Joseph Abuchi; Attama, Anthony Amaechi; Ugwu, Chinenye Nnenna; Ezeibe, Ezinwanne Nneoma; Momoh, Mumuni Audu; Echezona, Adaeze Chidiebere & Kenechukwu, Franklin Chimaobi
Background: Artemether and lumefantrine display low aqueous solubility leading to poor release profile; hence the need for
the use of lipid-based systems to improve their oral bioavailability so as to improve their therapeutic efficacy.
Aim and objective: The objective of this work was to utilize potentials of nanostructured lipid carriers (NLCs) for improvement
of the oral bioavailability of artemether and lumefantrine combination and to evaluate its efficacy in the treatment
of malaria. This study reports a method of formulation, characterization and evaluation of the therapeutic efficacies
of caprol-based NLC delivery systems with artemether and lumefantrine.
Method: The artemether-lumefantrine co-loaded NLCs were prepared using the lipid matrix (5% w/w) (containing beeswax
and Phospholipon® 90H and Caprol-PGE 860), artemether (0.1%w/w) and lumefantrine (0.6%w/w), sorbitol (4%w/w),
Tween® 80( 2%w/w as surfactant) and distilled water (q.s to 100%) by high shear homogenization and evaluated for physicochemical
performance. The in vivo antimalarial activities of the NLC were tested in chloroquine-sensitive strains of Plasmodium
berghei (NK-65) using Peter´s 4-day suppressive protocol in mice and compared with controls. Histopathological
studies were also carried out on major organs implicated in malaria.
Results: The NLC showed fairly polydispersed nano-sized formulation (z-average:188.6 nm; polydispersity index,
PDI=0.462) with no major interaction occurring between the components while the in vivo study showed a gradual but sustained
drug release from the NLC compared with that seen with chloroquine sulphate and Coartem®. Results of histopathological
investigations also revealed more organ damage with the untreated groups than groups treated with the formulations.
Conclusion: This study has shown the potential of caprol-based NLCs for significant improvement in oral bioavailability
and hence antimalarial activity of poorly soluble artemether and lumefantrine. Importantly, this would improve patient compliance
due to decrease in dosing frequency as a sustained release formulation.
Nanostructured lipid carriers; artemether-lumefantrine; malaria; Caprol.