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1
Fast Dissolving Oral Drug Delivery System Based on Electrospun Nanofibrous Webs of Cyclodextrin/Ibuprofen Inclusion Complex Nanofibers.基于环糊精/布洛芬包合物纳米纤维的静电纺丝纳米纤维网的快速溶解口腔给药系统。
Mol Pharm. 2019 Oct 7;16(10):4387-4398. doi: 10.1021/acs.molpharmaceut.9b00798. Epub 2019 Sep 4.
2
Fast dissolving oral films for drug delivery prepared from chitosan/pullulan electrospinning nanofibers.壳聚糖/普鲁兰电纺纳米纤维制备的速溶口腔膜用于药物传递。
Int J Biol Macromol. 2019 Sep 15;137:224-231. doi: 10.1016/j.ijbiomac.2019.06.224. Epub 2019 Jun 28.
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Fast-dissolving electrospun gelatin nanofibers encapsulating ciprofloxacin/cyclodextrin inclusion complex.快速溶解的电纺明胶纳米纤维包埋环糊精包合物中的环丙沙星。
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Continuous alternative to freeze drying: Manufacturing of cyclodextrin-based reconstitution powder from aqueous solution using scaled-up electrospinning.连续替代冷冻干燥:使用放大的静电纺丝从水溶液中制造基于环糊精的复溶粉末。
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Cyclodextrin⁻Drug Inclusion Complexes: In Vivo and In Vitro Approaches.环糊精-药物包合物:体内和体外方法。
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Electrospinning of Cyclodextrin Functional Nanofibers for Drug Delivery Applications.用于药物递送应用的环糊精功能化纳米纤维的静电纺丝
Pharmaceutics. 2018 Dec 24;11(1):6. doi: 10.3390/pharmaceutics11010006.
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Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review.静电纺丝技术制备的难溶性药物无定形固体分散体:综述
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Electrospun fixed dose formulations of amlodipine besylate and valsartan.静电纺固定剂量的苯磺酸氨氯地平和缬沙坦制剂。
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Fast dissolving drug delivery membrane based on the ultra-thin shell of electrospun core-shell nanofibers.基于电纺核壳纳米纤维超薄壳的速溶药物输送膜。
Eur J Pharm Sci. 2018 Sep 15;122:195-204. doi: 10.1016/j.ejps.2018.07.002. Epub 2018 Jul 3.
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用于快速溶解口服给药系统的氢化可的松/环糊精复合物电纺纳米纤维

Hydrocortisone/cyclodextrin complex electrospun nanofibers for a fast-dissolving oral drug delivery system.

作者信息

Celebioglu Asli, Uyar Tamer

机构信息

Department of Fiber Science & Apparel Design , College of Human Ecology , Cornell University , Ithaca , NY 14853 , USA . Email:

出版信息

RSC Med Chem. 2020 Jan 8;11(2):245-258. doi: 10.1039/c9md00390h. eCollection 2020 Feb 1.

DOI:10.1039/c9md00390h
PMID:33479631
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7484989/
Abstract

The electrospinning of hydrocortisone/cyclodextrin complex nanofibers was performed in order to develop a fast-dissolving oral drug delivery system. Hydrocortisone is a water-insoluble hydrophobic drug, yet, the water solubility of hydrocortisone was significantly enhanced by inclusion complexation with hydroxypropyl-beta-cyclodextrin (HP-β-CyD). In this study, hydrocortisone/HP-β-CyD complexes were prepared in aqueous solutions having molar ratios of 1/1, 1/1.5 and 1/2 (hydrocortisone/HP-β-CyD). Highly concentrated aqueous solutions of HP-β-CyD (180%, w/v) were used for hydrocortisone/HP-β-CyD systems (1/1, 1/1.5 and 1/2) in order to perform electrospinning without the use of an additional polymer matrix. The turbidity of hydrocortisone/HP-β-CyD (1/1 and 1/1.5) aqueous solutions indicated the presence of some uncomplexed crystals of hydrocortisone whereas the aqueous solution of hydrocortisone/HP-β-CyD (1/2) was homogeneous indicating that hydrocortisone becomes totally water-soluble by inclusion complexation with HP-β-CyD. Nonetheless, the electrospinning of hydrocortisone/HP-β-CyD systems (1/1, 1/1.5 and 1/2) successfully yielded defect-free uniform nanofibrous structures. Moreover, the electrospinning process was quite efficient that hydrocortisone was completely preserved without any loss yielding hydrocortisone/HP-β-CyD nanofibers having the initial molar ratios (1/1, 1/1.5 and 1/2). The structural and thermal characterization of the hydrocortisone/HP-β-CyD nanofibers revealed that hydrocortisone was totally inclusion complexed with HP-β-CyD and was in the amorphous state in hydrocortisone/HP-β-CyD (1/2) nanofibers whereas some uncomplexed crystalline hydrocortisone was present in hydrocortisone/HP-β-CyD (1/1 and 1/1.5) nanofibers. Nevertheless, hydrocortisone/HP-β-CyD (1/1, 1/1.5 and 1/2) complex aqueous systems were electrospun in the form of nanofibrous webs having a free-standing and flexible nature. The hydrocortisone/HP-β-CyD (1/1, 1/1.5 and 1/2) nanofibrous webs have shown fast-dissolving behavior in water or when they were in contact with artificial saliva. Yet, the hydrocortisone/HP-β-CyD (1/2) nanofibrous web dissolved more quickly than the hydrocortisone/HP-β-CyD (1/1 and 1/1.5) nanofibrous webs due to the full inclusion complexation and the amorphous state of hydrocortisone in this sample. In short, the results suggest that polymer-free electrospun nanofibrous webs produced from hydrocortisone/HP-β-CyD could be quite applicable for fast-dissolving oral drug delivery systems.

摘要

为开发一种速溶口服给药系统,进行了氢化可的松/环糊精复合纳米纤维的静电纺丝。氢化可的松是一种水不溶性疏水性药物,然而,通过与羟丙基-β-环糊精(HP-β-CyD)形成包合物,氢化可的松的水溶性显著提高。在本研究中,氢化可的松/HP-β-CyD复合物在摩尔比为1/1、1/1.5和1/2(氢化可的松/HP-β-CyD)的水溶液中制备。为了在不使用额外聚合物基质的情况下进行静电纺丝,HP-β-CyD的高浓度水溶液(180%,w/v)用于氢化可的松/HP-β-CyD体系(1/1、1/1.5和1/2)。氢化可的松/HP-β-CyD(1/1和1/1.5)水溶液的浊度表明存在一些未复合的氢化可的松晶体,而氢化可的松/HP-β-CyD(1/2)水溶液是均匀的,这表明氢化可的松通过与HP-β-CyD形成包合物而完全水溶。尽管如此,氢化可的松/HP-β-CyD体系(1/1、1/1.5和1/2)的静电纺丝成功地产生了无缺陷的均匀纳米纤维结构。此外,静电纺丝过程非常高效,氢化可的松完全保留,没有任何损失,得到了具有初始摩尔比(1/1、1/1.5和1/2)的氢化可的松/HP-β-CyD纳米纤维。氢化可的松/HP-β-CyD纳米纤维的结构和热表征表明,氢化可的松在氢化可的松/HP-β-CyD(1/2)纳米纤维中与HP-β-CyD完全形成包合物且处于无定形状态,而在氢化可的松/HP-β-CyD(1/1和1/1.5)纳米纤维中存在一些未复合的结晶氢化可的松。然而,氢化可的松/HP-β-CyD(1/1、1/1.5和1/2)复合水体系以具有自立性和柔韧性的纳米纤维网形式进行静电纺丝。氢化可的松/HP-β-CyD(1/1、1/1.5和1/2)纳米纤维网在水中或与人工唾液接触时表现出速溶行为。然而,由于该样品中氢化可的松的完全包合络合和无定形状态,氢化可的松/HP-β-CyD(1/2)纳米纤维网比氢化可的松/HP-β-CyD(1/1和1/1.5)纳米纤维网溶解得更快。简而言之,结果表明,由氢化可的松/HP-β-CyD制备的无聚合物静电纺纳米纤维网可非常适用于速溶口服给药系统。