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Preparation and characterization of paclitaxel-loaded DSPE-PEG-liquid crystalline nanoparticles (LCNPs) for improved bioavailability.

Abstract
Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as a new drug nanocarrier system for improving bioavailability for both hydrophilic and hydrophobic drugs. In this study, self-assembled LCNPs based on soy phosphatidyl choline and glycerol dioleate, which was known possessing low toxicity and negligible hemolysis, were prepared using poly(ethylene glycol)-grafted 1,2-distearoyl-sn-glycero-3-phosphatidylethanolamine (DSPE-PEG) as the dispersing agent. Paclitaxel (PTX) was used as a model hydrophobic drug. The particle size of the optimized DSPE-PEG-LCNPs and PTX-loaded DSPE-PEG-LCNPs were around 70nm. Crossed polarized light microscopy was used to characterize the phase behavior of liquid crystalline (LC) matrices, which showed a fan-like birefringent texture in dark background indicating the coexistence of reversed cubic and hexagonal phase in the optimized LC matrix. Transmission electron microscopy and cryo-field emission scanning electron microscopy revealed its internal water channel and "twig-like" surface morphology. PTX-loaded DSPE-PEG-LCNPs exhibited a biphasic drug sustained release pattern with a relatively fast release at the initial stage and a sustained release afterwards. PTX-loaded DSPE-PEG-LCNPs presented higher AUC (410.942±72.522μg/Lh) when compared with commercial product Taxol (212.670±41.396μg/Lh). These results indicated that DSPE-PEG-LCNPs might serve as a potential sustained release system for poorly water-soluble agents.
AuthorsNi Zeng, Quanyin Hu, Zhongyang Liu, Xiaoling Gao, Rongkuan Hu, Qingxiang Song, Guangzhi Gu, Huimin Xia, Lei Yao, Zhiqing Pang, Xinguo Jiang, Jun Chen, Liang Fang
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 424 Issue 1-2 Pg. 58-66 (Mar 15 2012) ISSN: 1873-3476 [Electronic] Netherlands
PMID22240390 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier B.V. All rights reserved.
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Drug Carriers
  • Phosphatidylethanolamines
  • polyethylene glycol-distearoylphosphatidylethanolamine
  • Polyethylene Glycols
  • Paclitaxel
Topics
  • Animals
  • Antineoplastic Agents, Phytogenic (chemistry, pharmacokinetics)
  • Area Under Curve
  • Biological Availability
  • Drug Carriers (chemistry, pharmacokinetics)
  • Male
  • Microscopy, Electron, Scanning
  • Microscopy, Electron, Transmission
  • Nanoparticles (chemistry, ultrastructure)
  • Paclitaxel (chemistry, pharmacokinetics)
  • Particle Size
  • Phosphatidylethanolamines (chemistry, pharmacokinetics)
  • Polyethylene Glycols (chemistry, pharmacokinetics)
  • Rats
  • Rats, Sprague-Dawley

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