Solid lipid nanoparticles for enhancing vinpocetine's oral bioavailability.
An ultrasonic-solvent emulsification technique was adopted to prepare vinpocetine loaded Glyceryl monostearate (GMS) nanodispersions with narrow size distribution. To increase the lipid load the process was conducted at 50 degrees C, and in order to prepare nanoparticle using an ultrasonic-solvent emulsification technique. The mean particle size and droplet size distribution, drug loading capacity, drug entrapment efficiency (EE%), zeta potential, and long-term physical stability of the SLNs were investigated in detail respectively. Drug release from two sorts of VIN-SLN was studied using a dialysis bag method. A pharmacokinetic study was conducted in male rats after oral administration of 10 mg kg(-1) VIN in different formulations, it was found that the relative bioavailability of VIN in SLNs was significantly increased compared with that of the VIN solution. The amount of surfactant also had a marked effect on the oral absorption of VIN with SLN formulations. The absorption mechanism of the SLN formulations was also discussed. These results indicated that VIN absorption is enhanced significantly by employing SLN formulations. SLNs offer a new approach to improve the oral bioavailability of poorly soluble drugs.
Luo
YiFan
Y
School of Pharmacy, Department of Pharmaceutics, Mailbox 42, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016 Liaoning, P.R. China.
Chen
DaWei
D
Ren
LiXiang
L
Zhao
XiuLi
X
Qin
Jing
J
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry*; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008297:Male; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D055672:Static Electricity; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D014748:Vinca Alkaloids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
D004337:Drug Carriers; D004655:Emulsions; D005989:Glycerides; D008055:Lipids; D010713:Phosphatidylcholines; D013501:Surface-Active Agents; D014665:Vasodilator Agents; D014748:Vinca Alkaloids; C048159:glyceryl monostearate; C013983:vinpocetine