ARTEMETHER LUMEFANTRINE LOADED LIPOSPHERES EVALUATION OF PROPERTIES OF SOLUTOL HS 15 AND SOLUPLUS ON THE IN VITRO PROPERTIES
To formulate artemether lumefantrine loaded lipospheres and to evaluate the effect of excipients on the in vitro properties
Materials and methods: Lipospheres were formulated using goat fat (70 percentage) and Phospholipon 90H (70 percentage) as the lipid matrix, Solutol HS 15 and Soluplus were used respectively as surfactants.Â The lipospheres were formulated by melt homogenization and analysed for drug content, encapsulation efficiency (EEpercentage), particle size and pH stability. In vitro release was studied in simulated gastric fluid (SGF, 1.2) and simulated intestinal fluid (SIF, 7.2). Â Â Â Â Â Â Results: Lipospheres formulated with Solutol had particle size range of 24.16 to 30.89 Î¼m, while those formulated with Soluplushad particle size range of 24.72 to 74.16 Î¼m. The formulations showed a decline in pH at 30 days. The EE of artemether range from 71.80 to 75.30 percentage for lipospheres formulated with Soluplus, while those formulated with Solutolhad EEpercentage of 65.30 to 75.02 percentage. Also, the EEpercentage of lumefantrine ranged from 76.36 to 88.99 percentage for lipospheres formulated with Soluplus, while those containing Solutolhad EE range of 73.22 to 85.06 percentage. Formulations exhibited sustained release properties with maximum release of at 6 h, however, lumefantrine exhibited higher release than artemether in SIF (p less than 0.05) and significantly lower release in SGF (p less than 0.05). Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Â Conclusion: Lipospheres exhibited good properties as a delivery system for artemether-lumefantrine.
Keywords: Goat fat, phospholipid, antimalaria, melt homogenization, loading capacity
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