Development of nanosuspension formulation for oral delivery of quercetin

J Biomed Nanotechnol. 2010 Aug;6(4):325-32. doi: 10.1166/jbn.2010.1133.

Abstract

With the aim to enhance dissolution rate and oral bioavailability of quercetin, a poorly water-soluble drug, quercetin loaded nanosuspension (QT-NS) was fabricated by a tandem of nano-precipitation (NP) and high pressure homogenization (HPH) method. The formulation of nanosuspension was optimized by screening different stabilizers. Characterization of the original QT powder and QT-NS was carried out by transmission electron microscopy and scanning electron microscopy, X-ray diffraction (XRD) and dissolution tests. QT-NS presented a sphere-like shape under transmission electron microscopy with an average diameter of 393.5 nm and the zeta potential of -35.75 mV. XRD study suggested that QT was maintained in the state of crystalline during the fabrication process. The solubility of QT in nanosuspension was about 70-fold that of crude QT, and the dissolution of QT from QT-NS was increased as compared to that of the original QT powder. In plasma, QT-NS exhibited a significant reduction of clearance rate (2 +/- 0.1 mL/min vs. 15 +/- 4 mL/min) and increase of AUC(0-infinity), (53995 +/- 4126 microg/mL x min versus 3470 +/- 110.1 microg/mL x min) compared with the control suspension. Our results showed that the developed nanosuspension formulation had a great potential as a possible formulation of the poorly water-soluble QT to enhance the bioavailability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Male
  • Microscopy, Electron, Transmission
  • Molecular Structure
  • Nanotechnology
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / chemistry
  • Polyethylene Glycols / chemistry
  • Propylene Glycols / chemistry
  • Quercetin / administration & dosage
  • Quercetin / chemistry*
  • Quercetin / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Solubility
  • Suspensions

Substances

  • PEO-PPO-PEO
  • Pharmaceutical Preparations
  • Propylene Glycols
  • Suspensions
  • Polyethylene Glycols
  • Quercetin