首页> 外文期刊>International Journal of Pharmaceutics >Inclusion complexes of isoflavones with two commercially available dendrimers: Solubility, stability, structures, release behaviors, cytotoxicity, and anti-oxidant activities
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Inclusion complexes of isoflavones with two commercially available dendrimers: Solubility, stability, structures, release behaviors, cytotoxicity, and anti-oxidant activities

机译:异黄酮与两种市售树状聚合物的包合物:溶解度,稳定性,结构,释放行为,细胞毒性和抗氧化活性

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We prepared and characterized the inclusion complexes of daidzein with poly(amidoamine) (PAMAM) and poly(propylene imine) (PPI) dendrimers. Aqueous solubility of daidzein was significantly enhanced by both PAMAM and PPI (186- and 650-fold at 0.36 mM, respectively). Daidzein in G3 PAMAM solution is more stable than that in G4 PPI. NMR studies reveal the encapsulation of daidzein within the interior cavities of PPI through hydrophobic interactions. Daidzein exhibits a slower release behavior from PPI than that from PAMAM. PPI/daidzein complex is much more toxic than PAMAM/daidzein complex on several cell lines. PAMAM/daidzein complexes showed similar protective effect on oxidative stress-induced cytotoxicity as compared to free daidzein. These results suggest that the inclusion of daidzein with dendrimer can effectively improve the solubility, prolong the delivery, and maintain the anti-oxidant activity of daidzein. This research provides new insights into dendrimer-based drug delivery systems and will be helpful for the design of novel dendrimer/drug formulations.
机译:我们制备并表征了大豆苷元与聚(酰胺基胺)(PAMAM)和聚(丙烯亚胺)(PPI)树状聚合物的包合物。 PAMAM和PPI均显着增强了大豆苷元的水溶性(在0.36 mM时分别为186倍和650倍)。 G3 PAMAM解决方案中的大豆苷元比G4 PPI更稳定。 NMR研究表明,黄豆苷元通过疏水作用在PPI的内部腔体内包封。大豆苷元从PPI的释放行为比从PAMAM的释放行为慢。在几种细胞系中,PPI /大豆苷元复合物的毒性比PAMAM /大豆苷元复合物的毒性大得多。与游离大豆苷元相比,PAMAM /大豆苷元复合物对氧化应激诱导的细胞毒性具有相似的保护作用。这些结果表明,黄豆苷元与树枝状聚合物的结合可以有效地提高黄豆苷元的溶解性,延长递送时间并保持黄豆苷元的抗氧化活性。这项研究为基于树枝状大分子的药物递送系统提供了新的见解,并将有助于设计新型树枝状大分子/药物制剂。

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