Development of Solid Lipid Nanoparticles for Enhanced Oral Bioavailability of Poorly Soluble Drugs

Abstract

The present study examines how solid lipid nanoparticles (SLNs) could increase paclitaxel's oral bioavailability. Soy lecithin, poloxamer 188, and stearylamine were used as emulsifiers in the modified solvent injection technique to create paclitaxel-loaded SLNs (PTX-SLNs). Surface morphology, size and size distribution, surface chemistry, and encapsulation effectiveness were used to characterize SLNs. Studies on the pharmacokinetics and bioavailability of PTX-SLNs administered orally to male Swiss albino mice were carried out. SLNs were spherical in form and had a smooth surface, according to transmission electron microscopy (TEM) analysis. With a zeta potential of 39.1±0.8 mV and a low polydispersity index of 0.162±0.04, the average particle size of SLNs was 96±4.4 nm. It was discovered that the loading capacity was 31.5±2.1% (w/w) and the drug entrapment effectiveness was 75.42±1.5%. Paclitaxel adhered to Higuchi kinetic equations and had a gradual and continuous in vitro release profile. When compared to free paclitaxel solution, drug exposure in plasma and tissues after oral administration of the PTX-SLNs was ten times and two times greater, respectively. In comparison to free paclitaxel solution (3,087 ng/ml), PTX-SLNs generated a high mean Cmax (10,274 ng/ml). It was discovered that the absorbed medication was dispersed throughout the brain, spleen, kidneys, liver, and lungs. According to in vivo toxicity investigations, the findings indicated that PTX-SLNs dispersed in an aqueous environment are potential new formulations that improved the oral bioavailability of hydrophobic medicines, such as paclitaxel, and were rather safe for oral administration of paclitaxel.