Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery

Arch Pharm Res. 2007 Sep;30(9):1138-43. doi: 10.1007/BF02980249.

Abstract

The purpose of the present study was to determine whether Pluronic F127 polymeric micelles could improve the oral bioavailability of a poor water-soluble drug, such as genistein. Genistein is a phytoestrogen that has estrogenic activity. F127 triblock copolymer consists of PEO100-PPO65-PEO100. Genistein was incorporated in the Pluronic F127 polymeric micelles by a solid dispersion method. The genistein release of genistein-loaded polymeric micelles was studied in vitro (in pH 1.2 and pH 6.8). And the oral bioavailabilities of genistein powder and genistein-loaded micelles were estimated at a dose of 4.0 mg/kg as genistein in rats. Drug loading amount and drug loading efficiency were 11.18% and 97.41%, respectively. The average size of the genistein-loaded polymeric micelles was 27.76 nm. And genistein release of the genistein-loaded polymeric micelles in vitro was 58% (pH 1.2) and 82% (pH 6.8). The bioavailability of genistein-loaded polymeric micelles was better than genistein powder. Consequently, Pluronic F127 polymeric micelles are an effective delivery system for the oral administration of genistein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Genistein / administration & dosage*
  • Genistein / chemistry
  • Genistein / pharmacokinetics
  • Hydrogen-Ion Concentration
  • Male
  • Micelles*
  • Particle Size
  • Poloxamer / administration & dosage*
  • Rats
  • Rats, Sprague-Dawley
  • Solubility

Substances

  • Micelles
  • Poloxamer
  • Genistein