Pharmacokinetics, tissue distribution and relative bioavailability of geniposide-solid lipid nanoparticles following oral administration.
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 Cmax value of geniposide in the geniposide-SLNs was significantly higher than that obtained with geniposide solution. Compared with the geniposide solution, the t1/2 and MRT were prolonged; the CL and V1/F were increased with geniposide-SLNs. The AUC0-∞values of geniposide-SLNs were 50 times greater than geniposide solution. The ratios of AUC0-8 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.
School of Pharmacy, Taishan Medical University , Taian , China.
Fugang
F
Wang
Juan
J
Cao
Jifu
J
Hao
Ke
K
Liu
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D039823:Iridoids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D009928:Organ Specificity / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley
D004337:Drug Carriers; D039823:Iridoids; D008055:Lipids; C007835:geniposide
Bioavailability; geniposide; geniposide-SLNs; pharmacokinetics; tissue distribution