Pharmacokinetics, tissue distribution and relative bioavailability of geniposide-solid lipid nanoparticles following oral administration

Abstract

Geniposide has various pharmacological effects; however, low oral bioavailability limits its clinical utility. This study explores the pharmacokinetics, tissue distribution and relative bioavailability of geniposide-solid lipid nanoparticles (SLNs) following oral administration. The geniposide solution and geniposide-SLNs were orally administered to the rats, respectively. The C_max value of geniposide in the geniposide-SLNs was significantly higher than that obtained with geniposide solution. Compared with the geniposide solution, the t_1/2 and MRT were prolonged; the CL and V1/F were increased with geniposide-SLNs. The AUC_0–∞values of geniposide-SLNs were 50 times greater than geniposide solution. The ratios of AUC_{0–8 h} in the liver, spleen, heart, kidney, brain and lung of the geniposide-SLNs to geniposide solution were 25.93, 4.28, 27.91, 10.15, 5.16 and 16.22, respectively. Prepared geniposide-SLNs are very helpful for increasing the bioavailability of geniposide. These data suggest that SLNs are a promising delivery system to enhance the oral bioavailability of geniposide.

• Bioavailability
• geniposide
• geniposide-SLNs
• pharmacokinetics
• tissue distribution