Development And Characterization Of Lyophilized Nanosuspension Containing Lumefantrine And Artemether

Abstract

The Aim of the present study is to solve water solubility concerns, newlineImprovement of oral bioavailability, dissolution rate and enhancement of permeability. newlineMaterial and Methods: An attempt done to perform coating of drugs using lecithin to newlineincrease solubility. Characterization of lecithin coated drugs were carried out. Stabilizer, surfactants and polymers incorporated to prepare nanosuspension by two approaches media milling method and anti-solvent precipitation-ultrasonication method followed by freeze dried using mannitol. Developed and validated RP-HPLC method used for estimation of drugs for In-vitro dissolution. Ex-vivo permeability using everted gut sac in rats HPLC-MS/MS method development and validation for quantitation of drugs in newlinerat plasma. In -vivo pharmacokinetics were evaluated in rats. newlineResults and Discussion: Lecithin coated drug FT-IR revealed absence of 3300 cm-1 newlinerespective to O-H stretching, due to complex formation at O-H group with drug and newlineabsence of signal at 4.5 ppm in 1H NMR. The optimized formulation has particle size newline(168.3 ± 3.7 nm) PDI (0.126± 0.05), zeta potential (and#8722;25.7 ± 0.9 mV). SEM analysis newlineillustrated the spherical shape of particles below 250 nm. Small particle size obtained newlinedue to presence of higher amount of beads increase in milling time in zirconium oxide newlinebead milling method. Increase in surfactant concentration with simultaneous increase newlinein sonication time, diminished particle size and decrease in t90 observed for anti-solvent precipitation-ultrasonication.Chromatographic separations with good resolutions in RP-HPLC method (Isocratic elution). Saturated solubility of nanosuspension in water increased ~ 6 times for LUF and ~5 times for ART. In-vitro dissolution and#707; 95% for both drugs in 15 minutes. The results of the GC analysis depicted presence of 10 ppm Chloroform. newline newline