title: Preparation and characterization of vinpocetine loaded nanostructured lipid carriers (NLC) for improved oral bioavailability.
abstract: 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.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China. chunyangzhuang@hotmail.com
authors.forename: Chun-Yang
authors.initials: CY
authors.lastname: Zhuang
authors.forename: Ning
authors.initials: N
authors.lastname: Li
authors.forename: Mi
authors.initials: M
authors.lastname: Wang
authors.forename: Xiao-Ning
authors.initials: XN
authors.lastname: Zhang
authors.forename: Wei-San
authors.initials: WS
authors.lastname: Pan
authors.forename: Jun-Jie
authors.initials: JJ
authors.lastname: Peng
authors.forename: Yu-Sheng
authors.initials: YS
authors.lastname: Pan
authors.forename: Xin
authors.initials: X
authors.lastname: Tang
mesh_terms: 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
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; D018697:Nootropic Agents; D014748:Vinca Alkaloids; C013983:vinpocetine