Formulation and Characterization of Solid Lipid Nanoparticles Containing Artemether and Lumefantrine for Treatment of P. falciparum

Abstract

Objective: To investigate sustained release of solid lipid nanoparticles containing Artemether and Lumefantrine against the P. falciparum by the combination of drugs that eventually will decrease the chance of drug resistance development. Methods: Artemether and Lumefantrine come under BCS class II (poor aqueous solubility and high permeability) and these drug molecules possess low oral bioavailability due to improper dissolution and incomplete absorption. Novel formulation of Artemether and Lumefantrine may eliminate all of shortcomings and may lead to enhance oral bioavailability due to increase in solubility of these drugs. Liquid crystalline nanoparticles (cubosomes or hexosomes) containing Artemether and Lumefantrine were formulated by Hydrotropic dilution method. In this method ethanolic solution of GMO with drug and aqueous solution of Poloxamer 407 were prepared by vortexing. Water phase containing the Poloxamer (10% w/v) added to the ethanolic phase drop wise with continuously vortexing resulting in the precipitation of the GMO. A milky suspension is formed which indicate the formation of liquid crystallineas Results: The average particle size of Artemether and Lumefantrine loaded SLNs decreased with increasing concentration of surfactant. SLNs of 193.5-194 nm with a Polydispersity index of (0.600 ± 0.10) were obtained at higher concentration of lipid and surfactant. Entrapment efficiency of Artemether and Lumefantrine were found 85% and 95.5% insolid lipid nanoparticles. Furthermore the stability of SLNs indicated with negligible drug leakage after 3 weeks in stability studies as per ICH guidelines. Physical and chemical stability study revealed no major change in particle size and entrapment efficiency of liquid crystalline nanoparticles. Conclusion: The result concluded that Artemether and Lumefantrine were loaded in solid lipid nanoparticles that exhibited sustained release from the designed dosage form against the P. falciparum and decrease the chances of drug resistance development during the treatment.