Formulation, In vitro and In vivo Evaluation of Sustained released ArtemetherLumefantrine-Loaded microstructured solid Lipid Microparticles (SLMs) doi.org/10.26538/tjnpr/v5i8.23
Main Article Content
Abstract
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.
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