Solid Lipid Nanoparticles of Sulpiride: Improvement of Pharmacokinetic Properties

Abstract

Objectives: In this study, it is hypothesized that lipid carriers could enhance the pharmacokinetic behaviour of Sulpiride (Sul). Different Lipids such as Palmitic Acid (PA), Stearic Acid (SA) and triaplmitin (TA) were used to prepare Solid Lipid Nanoparticles (SLNs) which is then better characterized and tested for its in vivo bioavailability. Methods: SLNs were prepared using film homogenization technique. Different physicochemical parameters such as Homogenization Speed (HS), Homogenization Time (HT) and Sonication Time (ST) were evaluated. Surfactant type and concentration of surfactant, soy lecithin and lipid type were scrutinized. Finally, SLNs pharmacokinetic parameters were evaluated. Results: Sul Entrapment Efficiency (EE) and drug loading were highly associated with solubility in lipid and partition coefficients. The particle size was decreased with an increase in HT, HS and ST. According to lipid type, the EE was high using SA and low using TP. The EE was raised with an increment in the concentration of lipids and soy lecithin. Regarding the in vivo study, Sul SLNs showed 2.64 fold increase in relative bioavailability with higher Cmax (816.22 ng/ml) than the drug suspension form (550 ng/ml). Conclusion: SLNs are considered promising flexible carriers that can be tailored to enhance the solubility, bioavailability and the expected therapeutic response of poorly soluble drugs.