Abstract
To optimize a nanostructured lipid carriers system (NLC) for the per-oral delivery of valsartan (Val), a model BCS class II drug, in an attempt to enhance its therapeutic performance by increasing both solubility and dissolution. Val-loaded NLCs were prepared using ultrasonic melt-emulsification method. Number of formulation factors including the type of oil/lipid, Val to lipid ratio, and surfactant ratio were investigated. The prepared NLC were evaluated for their particle size and shape, polydispersity index, zeta potential, and drug entrapment efficiency. The in vitro drug release profiles were evaluated using a dialysis bags with cut-off 12KD. The prepared NLCs showed average sizes between 423.99 +/- 12.73 and 805.53 +/- 39.5 nm, and polydispersity index in the range of 0.287 to 0.361. The zeta-potential values were between -3.34 and -10.59 mV. The entrapment efficiency was not very high between 27.3 to 75.04%. The scanning electron images showed almost spherical shapes with sizes lower than those obtained by light scattering. The in vitro release followed a bi-phasic pattern with an initial rapid Val release followed by a slow release varying according to the composition. Two formulations F2 and F4 showed complete drug release within the first two hours. The optimum surfactant ratio was 37.5% by weight of the total lipid. NLC successfully enhanced the Val release rate and dissolution with high potential to enhance its bioavailability.