Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery

• Published in: Archives of pharmacal research 2007, 30(9), , pp.1138-1143
• Main Authors: 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, Sangkil, Chang, Jung Yun, Lee, Jaehwi, Choi, Young Wook
• Format: Article
• Language: English
• Subjects: 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; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/bf02980249

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.