International Journal of Nanomedicine, 2011, 6(1):2429-35.

Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Jingling Tang, Na Xu, Hongyu Ji , et al

Department of Pharmacy, the Second Affiliated Hospital of Harbin Medical University, Key Laboratory of College in Heilongjiang Province; Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, China

Background      

Genistein, one of the major isoflavones, has received great attention as a phytoestrogen and potential cancer chemoprevention agent. However, the dissolution and bioavailability of genistein from solid oral preparations is low due to its poor water solubility.

Methods

In order to improve the oral bioavailability of genistein, genistein nanoparticles were prepared by the nanoprecipitation technique using Eudragit® E100 as carriers and an optimized formulation of mass ratio (genistein:Eudragit E100, 1:10). The mean particle size of genistein nanoparticles was approximately 120 nm when diluted 100 times with distilled water. The drug-loaded nanoparticles were spherical on observation by transmission electric microscopy.

Results

Encapsulation efficiency and drug loading of the genistein nanoparticles were approximately 50.61% and 5.02%, respectively. Release of drug from the genistein nanoparticles was two times greater than that from the conventional capsules. After administration of genistein suspension or genistein nanoparticles at a single dose of 100 mg/kg to fasted rats, the relative bioavailability of genistein from the nanoparticles compared with the reference suspension was 241.8%.

Conclusion

These results suggested that a nanoparticle system is a potentially promising formulation for the efficient delivery of poorly water-soluble drugs by oral administration.

新西兰《纳米药物国际杂志》，2011年10月

包含金雀异黄素的丙烯酸树脂纳米颗粒︰ 配方、 研制和生物利用度测试

唐静玲，徐娜，季宏宇等

中国黑龙江省哈尔滨医科大学第二附属医院药学系，哈尔滨医科大学药剂学系

背景：

染料木黄酮，是主要的一种大豆异黄酮，作为植物雌激素和潜在的癌症化学预防试剂得到极大的关注。然而，由于其水溶性差，导致染料木素固体口服制剂的溶解度和生物利用度较低。

方法

为了提高染料木黄酮的口服生物利用度，使用 Eudragit® E100 作为载体，并且优化的配方质量比 (金雀异黄素:Eudragit E100为1:10) 通过纳米沉淀技术制备金雀异黄素纳米粒子。用蒸馏水稀释 100 倍时金雀异黄素纳米颗粒的平均粒径大约为 120 nm 。用透射电镜观察载药纳米颗粒呈现球形。

结果

封装效率和染料木素纳米颗粒载药量，分别为约 50.61%和 5.02%。金雀异黄素纳米颗粒的药物释放量是常规胶囊的两倍。以 100mg/kg单剂量对禁食大鼠给药金雀异黄素悬浮物或金雀异黄素纳米颗粒后, 与参照悬浮液相比，染料木素纳米颗粒的相对生物利用度为241.8%。

结论

这些结果表明，纳米粒子体系可能是一种有效输送难溶性药物口服给药有前景的配方。