Formulation and in vitro evaluation of quercetin loaded polymeric micelles composed of pluronic P123 and D-a-tocopheryl polyethylene glycol succinate

J Biomed Nanotechnol. 2011 Jun;7(3):358-65. doi: 10.1166/jbn.2011.1298.

Abstract

The objective of this study was to develop a polymeric delivery system to improve the solubility and biological activity of Quercetin (QT). QT loaded mixed micelles, composed of Pluronic P123 (P123) and D-a-tocopheryl polyethylene glycol succinate (TPGS) with proportion of 7:3 (QT-P/T), were prepared by thin-film hydration method. The average size of the mixed micelles was 18.43 nm, and the encapsulating efficiency for QT was 88.94 +/- 3.71%, drug-loading was 10.59 +/- 0.38%. The solubility of QT in QT-P/T was 5.56 mg/mL, which was about 2738-fold that of crude QT in water. Compared with the QT propylene glycol solution, the in vitro release of QT from QT-P/T presented the sustained-release property. The in vitro cytotoxicity assay showed that the IC50 values on MCF-7 cells for QT-P/T and QT loaded P123 micelles (QT-P123) were 7.13 microg/mL and 10.73 microg/mL, respectively, while 7.23 microg/mL and 14.47 microg/mL on MCF-7/ADR cells. From the results, it can be concluded that, P123/TPGS mixed micelles may serve as a pharmaceutical nano carrier with improved solubility and biological activity for QT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Breast Neoplasms / drug therapy
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chemistry, Pharmaceutical
  • Drug Delivery Systems
  • Female
  • Humans
  • Inhibitory Concentration 50
  • Micelles*
  • Microscopy, Electron, Transmission
  • Molecular Structure
  • Particle Size
  • Poloxalene* / chemistry
  • Polyethylenes* / chemistry
  • Quercetin / pharmacology*
  • Succinates* / chemistry
  • Tocopherols / pharmacology*

Substances

  • Antineoplastic Agents
  • Micelles
  • Polyethylenes
  • Succinates
  • poly(ethylene succinate)
  • pluronic block copolymer P123
  • Poloxalene
  • Quercetin
  • Tocopherols