Preparation and characterization of solid lipid nanoparticles loaded with alpha-Asarone.
This work investigated the potential of solid lipid nanoparticles (SLNs) to improve oral bioavailablity and tissue uptake of a poorly soluble drug, alpha-Asarone. Ultrasonic homogenization method was employed to prepare alpha-Asarone-loaded SLNs (alpha-Asarone-SLNs). Particle size and distribution, pH, viscosity, drug incorporation and zeta potential of the SLNs were investigated. Pharmacokinetic study of oral administration to male rats at 10 mg/Kg suggested that the relative bioavailability of alpha-Asarone was significantly improved in alpha-Asarone-SLN group compared to alpha-Asarone solution group. Comparison of alpha-Asarone-SLN to alpha-Asarone control solution for alpha-Asarone concentrations in rat tissue showed an increased uptake of alpha-Asarone in brain and lung for the ARE-SLN group. These results indicate that alpha-Asarone-SLNs significantly enhance the absorption and tissue distribution of alpha-Asarone. SLNs offer a new approach to improve the oral bioavailability of poorly soluble drugs.
Wang
Dongkai
D
Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China. sterlinghawk@126.com
Wang
Xiaoyan
X
Li
Xiang
X
Ye
Linmao
L
D000081248:Allylbenzene Derivatives; D000818:Animals; D000840:Anisoles / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D005343:Fibrinolytic Agents / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D008297:Male; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
D000081248:Allylbenzene Derivatives; D000840:Anisoles; D005343:Fibrinolytic Agents; C012195:asarone