title: Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery.
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.
authors.affiliation: Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, Seoul 156-756, Korea.
authors.forename: Suk Hyung
authors.initials: SH
authors.lastname: Kwon
authors.forename: Sun Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Kyoung Wook
authors.initials: KW
authors.lastname: Ha
authors.forename: Myung Joo
authors.initials: MJ
authors.lastname: Kang
authors.forename: Jin Seo
authors.initials: JS
authors.lastname: Huh
authors.forename: Tae Jong
authors.initials: TJ
authors.lastname: Im
authors.forename: Yong Min
authors.initials: YM
authors.lastname: Kim
authors.forename: Young Mi
authors.initials: YM
authors.lastname: Park
authors.forename: Kyoung Hoon
authors.initials: KH
authors.lastname: Kang
authors.forename: Sangkil
authors.initials: S
authors.lastname: Lee
authors.forename: Jung Yun
authors.initials: JY
authors.lastname: Chang
authors.forename: Jaehwi
authors.initials: J
authors.lastname: Lee
authors.forename: Young Wook
authors.initials: YW
authors.lastname: Choi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019833:Genistein / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D006863:Hydrogen-Ion Concentration; D008297:Male; D008823:Micelles; D010316:Particle Size; D020442:Poloxamer / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D008823:Micelles; D020442:Poloxamer; D019833:Genistein