Optimized Artemether-loaded Anhydrous Emulsion.
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Date
2014-01
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Abstract
Objective: The objectives of this study were to identify stable anhydrous emulsions via
pseudo ternary phase diagram, optimize artemether-loaded batches using factorial design
and subsequently evaluate the antimalarial activity.
Methodology: Using labrasol®, triacetin® and lauroglycol 90® as the surfactant, oil and
co-surfactant respectively, pseudo ternary phase diagram was generated from the
quantitative titration of water with the anhydrous emulsion. Stable combinations from the
phase diagram were subjected to a 23 full factorial experimental design. The 22 softwaregenerated
formulations were experimentally formulated and characterized for droplet size,
polydispersity index, viscosity and thermodynamic stability. Droplet size was chosen and
subsequently fitted into the Response column of the software, thus prompting the
generation of graphs and Desirability table of 125 predicted formulations. Out of the 125
predictions, three with the least droplet sizes (less than 100 nm) were adjudged as optimized batches. Subsequently, they were formulated, converted to powder by
adsorption on magnesium aluminum metasilicate and evaluated. Antimalarial
effectiveness of the drug-loaded formulation was also investigated.
Results: Triacetin® most significantly (P<0.05) contributed to droplet size variation. The
droplet size of the experimental formulations approximated that of the statistical
predictions. The anhydrous emulsions (AEs) were powderable and the granulations rated
fair and passable according to Carr’s scale. Artemether-loaded anhydrous emulsion (AE)
demonstrated highest antimalarial activity.
Conclusion: We therefore conclude that optimization proved a useful tool for the
identification of excipient proportions with optimal effects.
Description
Keywords
Anhydrous emulsion, optimized, pseudoternary phase diagram, droplet size, Flow properties, antimalarial activity
Citation
Obitte N C, Rohan L C, Adeyeye C M, Esimone C O. Optimized Artemether-loaded Anhydrous Emulsion. British Journal of Pharmaceutical Research. 2014 Jan; 4(1): 37-59.