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将芒柄花素/甲基-β-环糊精包合物嵌入到电纺聚乙烯醇纳米纤维中:提高了水溶解度和口服速溶性能。

Formononetin/methyl-β-cyclodextrin inclusion complex incorporated into electrospun polyvinyl-alcohol nanofibers: Enhanced water solubility and oral fast-dissolving property.

机构信息

School of Food Science and Biotechnology, Zhejiang Gongshang University, Xuezheng Street No. 18, Hangzhou 310018, China.

School of Food Science and Biotechnology, Zhejiang Gongshang University, Xuezheng Street No. 18, Hangzhou 310018, China.

出版信息

Int J Pharm. 2021 Jun 15;603:120696. doi: 10.1016/j.ijpharm.2021.120696. Epub 2021 May 11.

Abstract

Improving solubility and administration route of isoflavone formononetin (FMN) are critical factors to improve its bioavailability in the oral cavity. This study fabricated fast-dissolving nanofibers containing FMN/methyl-β-cyclodextrin (FMN/Me-β-CD) inclusion complex. The solubility of FMN could be increased by approximately 50 times at 20 mM aqueous Me-β-CD. Interactions and thermodynamic parameters of the host-guest inclusion complex were studied by a fluorescence quenching method. The structure and mechanisms of the complex were further studied by molecular docking and molecular dynamics. Finally, polyvinyl-alcohol (PVA) nanofibrous webs containing the FMN/Me-β-CD inclusion complex were fabricated by electrospinning. The dissolution test demonstrated that the FMN/Me-β-CD/PVA nanofibers can be dissolved in artificial saliva within approximately 2 s. This study shows the potential of Me-β-CD inclusion and electrospinning to improve solubility and administration route of isoflavones.

摘要

提高异黄酮芒柄花素(FMN)的溶解度和给药途径是提高其口腔生物利用度的关键因素。本研究制备了含有 FMN/甲基-β-环糊精(FMN/Me-β-CD)包合复合物的速溶纳米纤维。在 20mM 水合 Me-β-CD 中,FMN 的溶解度可提高约 50 倍。通过荧光猝灭法研究了主客体包合复合物的相互作用和热力学参数。通过分子对接和分子动力学进一步研究了复合物的结构和机制。最后,通过静电纺丝制备了含有 FMN/Me-β-CD 包合复合物的聚乙烯醇(PVA)纳米纤维网。溶解试验表明,FMN/Me-β-CD/PVA 纳米纤维可在大约 2s 内在人工唾液中溶解。本研究表明 Me-β-CD 包合和静电纺丝具有提高异黄酮溶解度和给药途径的潜力。

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