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KMID : 0043320070300091138
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Archives of Pharmacal Research
2007 Volume.30 No. 9 p.1138 ~ p.1143
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Pharmaceutical Evaluation of Genistein-loaded Pluronic Micelles for Oral Delivery
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Kwon Suk-Hyung
Kim Sun-Young
Ha Kyoung-Wook
Kang Myung-Joo
Huh Jin-Seo
Im Tae-Jong
Kim Yong-Min
Park Young-Mi
Kang Kyoung-Hoon
Lee Sang-kil
Chang Jung-Yun
Lee Jae-Hwi
Choi Young-Wook
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Abstract
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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 genisteinloaded 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
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KEYWORD
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Genistein, Polymeric micelles, Oral delivery, Pluronic, Bioavailability, Solubilization
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