Preparation and characterization of vinpocetine loaded nanostructured lipid carriers (NLC) for improved oral bioavailability.
The purpose of this study is to develop an optimized nanostructured lipid carriers (NLC) formulation for vinpocetine (VIN), and to estimate the potential of NLC as oral delivery system for poorly water-soluble drug. In this work, VIN-loaded NLC (VIN-NLC) was prepared by a high pressure homogenization method. The VIN-NLC showed spherical morphology with smooth surface under transmission electron microscope (TEM) and scanning electron microscopic (SEM) analysis. The average encapsulation efficiency was 94.9+/-0.4%. The crystallization of drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC). The drug was in an amorphous state in the NLC matrix. In the in vitro release study, VIN-NLC showed a sustained release profile of VIN and no obviously burst release was observed. The oral bioavailability study of VIN was carried out using Wistar rats. The relative bioavailability of VIN-NLC was 322% compared with VIN suspension. In conclusion, the NLC formulation remarkably improved the oral bioavailability of VIN and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs.
Zhuang
Chun-Yang
CY
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China. chunyangzhuang@hotmail.com
Li
Ning
N
Wang
Mi
M
Zhang
Xiao-Ning
XN
Pan
Wei-San
WS
Peng
Jun-Jie
JJ
Pan
Yu-Sheng
YS
Tang
Xin
X
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D018697:Nootropic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D014748:Vinca Alkaloids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; D018697:Nootropic Agents; D014748:Vinca Alkaloids; C013983:vinpocetine