Genistein-loaded poloxamer 403/407 mixed micelles: preparation and pharmacokinetic study in rats

作     者：Yan Cai Wei Dai Fuhua Qin Jieyin Sun Ruilong Wei 蔡雁;戴巍;钦富华;孙洁胤;魏瑞龙

作者机构：Department of Pharmacy Ningbo NO. 9 Hospital Ningbo 315020 China Department of Pharmeucital Engineering Zhejiang Pharmaceutical College Ningbo 315100 China Hangzhou Dongxiang Pharmaceutical Technology Co. Ltd. Hangzhou 310051 China 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2018年第27卷第5期

页      面：342-351页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：The Zhejiang Public Welfare Technology Application Research Project(Grant No.2015C31100) the Ningbo Science and Technology Innovation Team Project(Grant No.2015C110027) 

主　　题：Genistein Poloxamer 407 Poloxamer 403 Micelles Pharmacokinetics 

摘      要：In the present study, we aimed to prepare poloxamer 403/407 mixed micelles in order to improve the solubility and oral bioavailability of genistein. Genistein was incorporated in the mixed poloxamer micelles by thin-film hydration method, and its physicochemical properties, including particle size, zeta potential, entrapment efficiency and drug loading, were investigated. In vitro release of genistein from the mixed micelles was monitored by dialysis method, and pharmacokinetic study of genistein loaded mixed micelles was carried out in rats. We found that the particle size and zeta potential of mixed micelles were（20.31±0.43） nm and（–8.94±0.35） m V, with encapsulation efficiency 90.59%±0.67% and drug loading 7.74%±0.05%. Solubility of genistein in mixed micelles reached 3.80 mg/m L, which was about 130 times higher than that in water. Genistein-loaded mixed micelles showed sustained release characteristics in vitro with no burst release phenomenon, but it was faster than suspension. The AUC0–t and AUC0–∞ of mixed micelles were 196.74% and 204.62% greater than that of genisein suspension, respectively. Consequently, poloxamer 403/407 mixed micelles significantly improved the solubility and oral bioavailability of genistein, which could be used as an effective drug delivery system for oral administration of poorly soluble drugs.