Pravastatin-Loaded nanostructured lipid carriers: formulation optimization and in-vivo assessment for antihyperlipidaemic effect in rats

This study aimed to create nanostructured lipid carriers (NLCs) loaded with pravastatin to improve its long-term anti-hyperlipidemic effects. Preformulation research was conducted. High-shear homogenisation and ultrasonication were used to prepare NLCs containing stearic acid (solid lipid), oleic acid (liquid lipid), and varying amounts of Tween 80 and Poloxamer 188 as surfactants. Nine formulations were prepared using a 3² factorial design and evaluated for size, zeta, scanning electron microscopy, entrapment efficiency, release, and kinetics. The optimum formulation was further evaluated for <i>in vivo</i> antihyperlipidemic activity in rats, and the <i>in vitro</i> release profile and stability of the commercial preparation were assessed. The optimised formulation (F4) exhibited an entrapment efficiency of 98.35%, a zeta potential of -65.9 mV, and a particle size of 203.0 nm. Scanning electron microscopy revealed that the particles were spherical and exhibited sustained <i>in vitro</i> drug release (96.4% over 12 h). <i>In vivo</i> evaluation in hyperlipidemic Wistar rats showed significantly improved lipid profiles and reduced oxidative stress compared to marketed pravastatin tablets. Stability studies confirmed that the formulation was stable under various conditions, and release studies showed sustained release compared with the marketed formulation. These findings suggest that pravastatin-loaded NLCs are promising sustained-release systems for improved management of hyperlipidaemia.