Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery.
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.
Kwon
Suk Hyung
SH
Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, Seoul 156-756, Korea.
Kim
Sun Young
SY
Ha
Kyoung Wook
KW
Kang
Myung Joo
MJ
Huh
Jin Seo
JS
Im
Tae Jong
TJ
Kim
Yong Min
YM
Park
Young Mi
YM
Kang
Kyoung Hoon
KH
Lee
Sangkil
S
Chang
Jung Yun
JY
Lee
Jaehwi
J
Choi
Young Wook
YW
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
D008823:Micelles; D020442:Poloxamer; D019833:Genistein