PDF(Pubmed)
Abstract：
To address the prevalent genistein (GST) metabolism and inadequate intestinal absorption, an oral long-acting and gastric in-situ gelling gel was designed to encapsulate and localize the intestinal release of the loaded genistein-ginseng (GST-GNS) solid dispersion. Because of the high breast perfusion of GST upon oral absorption, the GST-GNS solid dispersion was developed to enhance GST\'s dissolution and penetration while offering a synergistic impact against breast cancer (BC). Physiochemical analysis of the GST-GNS solid dispersion, release analysis, gel characterizations, storage stability, penetration, and in vitro cytotoxicity studies were carried out. GST-GNS solid dispersion showed improved dissolution and penetration as compared to raw GST. GST-GNS solid dispersion homogenous shape particles and hydrophilic contacts were revealed by scanning electron microscopy and Fourier Transform-Infrared analysis, respectively. GST-GNS solid dispersion\'s diffractogram shows the amorphous character. A second modification involved creating a gastric in-situ gelling system loaded with GST-GNS solid dispersion. This system demonstrated improved GST penetration employing the solid dispersion, as well as the localizing of the GST release at the intestinal media and antitumor synergism against BC. For a better therapeutic approach for BC, the innovative oral GST long-acting gel encasing the GST-GNS solid dispersion would be recommended.
摘要：
为了解决普遍存在的染料木素（GST）代谢和肠道吸收不足，设计了一种口服长效和胃原位胶凝凝胶，用于包封和定位负载的染料木黄酮-人参（GST-GNS）固体分散体的肠道释放。由于口服吸收时GST的高乳房灌注，开发GST-GNS固体分散体可增强GST的溶解和渗透，同时对乳腺癌（BC）具有协同作用。GST-GNS固体分散体的生理化学分析，发布分析,凝胶表征，储存稳定性，穿透力,并进行了体外细胞毒性研究。与原始GST相比,GST-GNS固体分散体显示出改善的溶解和渗透。通过扫描电子显微镜和傅里叶变换-红外分析揭示了GST-GNS固体分散体均一形状颗粒和亲水接触,分别。GST-GNS固体分散体的衍射图显示无定形特征。第二种改进涉及产生装载有GST-GNS固体分散体的胃原位胶凝系统。该系统证明了使用固体分散体改善的GST渗透，以及GST在肠道介质中的局部释放和针对BC的抗肿瘤协同作用。为了更好的治疗BC，建议使用包含GST-GNS固体分散体的创新口服GST长效凝胶。
