Formulation, In vitro and In vivo Evaluation of Sustained released Artemether-Lumefantrine-Loaded microstructured solid Lipid Microparticles (SLMs)

 John D.N Ogbonna, Adaeze C. Echezona*, Chinekwu S. Nwagwu, Chinazom P. Agbo, Adaeze L. Onugwu, Franklin C. Kenechukwu, Paul A. Akpa, Mumuni A. Momoh, Anthony A. Attama
Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, University of Nigeria, Nsukka, 410001, Nigeria

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Recieved Date: 19 March 2021; Accepted Date: 19 August ; Published Date: 03 September
Citation: Ogbonna JDN, Echezona AC, Nwagwu CS, Agbo CP, Onugwu AL, Kenechukwu FC, Akpa PA, Momoh MA, Attama AA. Formulation, In vitro and In vivo Evaluation of Sustainedreleased Artemether-Lumefantrine-Loadedmicrostructuredsolid Lipid Microparticles (SLMs). Trop J Nat Prod Res. 2021; 5(8):1460-1469.
© 2021 Ogbonna et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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Owing to the low solubility of artemether which reduces its bioavailability, the study aimed at improving the solubility of artemether, in combination with lumefantrine loaded in a solid lipid microparticles (SLMs) using Capra hircus as the delivery carrier. Artemether-lumefantrine-loaded SLMs [(AL-loaded; AL0, AL1, AL2 and AL3 are 0, 3, 5 and 7% AL loaded respectively)] were prepared using hot homogenization, thereafter lyophilized and characterized. In vitro release of A-L was performed in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF) while the in vivo study was carried out using Peter’s Four days protocol after which the mice were subjected to histological studies. A pH stable SLMs, particle size of 9.15 ± 0.18 -23.67 ± 0.45 µm with high entrapment efficiency of lumefantrine than artemether was obtained. The release profile of the SLMs were pH-dependent, SGF (90%) and SIF (50%). The optimized SLMs had percentage parasitemia reduction (87.01%) that is significantly different from the commercial samples (80%) in Plasmodium berghi infected mice albeit not to a significant extent. Post-treatment haematological parameters showed that there was a significant difference (p ? 0.05) only in the PCV of group A (SLMs containing 3% of AL treated) and group B (commercial sample treated). The histological studies revealed that the SLMs formulations had no deleterious effects on the kidney and liver of the mice. Therefore, SLMs formulation might be an alternative means of delivering artemisinin combinations as stability and therapeutic efficacy were achieved without any significant harmful effect on the vital organs.

Keywords: Solid Lipid Microparticles, Plasmodium berghi, artemether-lumefantrine, parasitemia, haematological parameters, histological studies.
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ISSN: 2616-0684 (Print)
ISSN: 2616-0692 (Online)
DOI: 10.26538/tjnpr
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