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由磺丁基醚-β-环糊精(SBE-β-CD)与磺胺异噁唑形成的包合物制备的无聚合物电纺纳米纤维:磺胺异噁唑的快速溶解及水溶性增强

Polymer-free electrospun nanofibers from sulfobutyl ether-beta-cyclodextrin (SBE-β-CD) inclusion complex with sulfisoxazole: Fast-dissolving and enhanced water-solubility of sulfisoxazole.

作者信息

Yildiz Zehra Irem, Celebioglu Asli, Uyar Tamer

机构信息

Institute of Materials Science & Nanotechnology, UNAM-National Nanotechnology Research Center, Bilkent University, Ankara 06800, Turkey.

Institute of Materials Science & Nanotechnology, UNAM-National Nanotechnology Research Center, Bilkent University, Ankara 06800, Turkey.

出版信息

Int J Pharm. 2017 Oct 15;531(2):550-558. doi: 10.1016/j.ijpharm.2017.04.047. Epub 2017 Apr 23.

DOI:10.1016/j.ijpharm.2017.04.047
PMID:28445768
Abstract

In this study, our aim was to develop solid drug-cyclodextrin inclusion complex system having nanofibrous morphology in order to have fast-dissolving property and enhanced water-solubility of poorly water-soluble drug. Here, we prepared a highly concentrated aqueous solution of inclusion complex between sulfisoxazole and sulfobutyl ether-beta-cyclodextrin (SBE-β-CD, Captisol), and then, without using any polymeric matrix, the electrospinning of sulfisoxazole/SBE-β-CD-IC nanofibers was performed in order to obtain free-standing and handy nanofibrous web. As a control sample, nanofibers from pure SBE-β-CD was also electrospun and free-standing nanofibrous web was obtained. The SEM imaging revealed that the bead-free and uniform nanofiber morphology with the average fiber diameter (AFD) of 650±290nm for sulfisoxazole/SBE-β-CD-IC NF and 890±415nm for pure SBE-β-CD NF was obtained. The inclusion complex formation between sulfisoxazole and SBE-β-CD in sulfisoxazole/SBE-β-CD-IC NF sample was confirmed by H NMR, TGA, DSC, XRD and FTIR analyses. Due to the combined advantage of cyclodextrin inclusion complexation and high surface area of electrospun nanofibers, fast-dissolving property with enhanced water-solubility was successfully achieved for sulfisoxazole/SBE-β-CD-IC NF. Our findings suggest that electrospun nanofibers/nanowebs from CD-IC of poorly water-soluble drugs may offer applicable approaches for high water-solubility and fast-dissolving tablet formulations for drug delivery systems.

摘要

在本研究中,我们的目标是开发具有纳米纤维形态的固体药物 - 环糊精包合物体系,以实现难溶性药物的快速溶解性能并提高其水溶性。在此,我们制备了磺胺异恶唑与磺丁基醚 -β-环糊精(SBE-β-CD,Captisol)之间包合物的高浓度水溶液,然后在不使用任何聚合物基质的情况下,进行磺胺异恶唑/SBE-β-CD-IC纳米纤维的静电纺丝,以获得独立且方便的纳米纤维网。作为对照样品,也对纯SBE-β-CD进行了静电纺丝并获得了独立的纳米纤维网。扫描电子显微镜成像显示,磺胺异恶唑/SBE-β-CD-IC纳米纤维的平均纤维直径(AFD)为650±290nm,纯SBE-β-CD纳米纤维的平均纤维直径为890±415nm,均获得了无珠且均匀的纳米纤维形态。通过1H NMR、TGA、DSC、XRD和FTIR分析证实了磺胺异恶唑/SBE-β-CD-IC纳米纤维样品中磺胺异恶唑与SBE-β-CD之间形成了包合物。由于环糊精包合作用和静电纺纳米纤维高比表面积的综合优势,磺胺异恶唑/SBE-β-CD-IC纳米纤维成功实现了具有增强水溶性的快速溶解性能。我们的研究结果表明,难溶性药物的环糊精包合物静电纺纳米纤维/纳米网可为药物递送系统的高水溶性和快速溶解片剂配方提供适用方法。

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