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[通过电纺载药纳米纤维提高难溶性药物的溶解度]

[The improvement of poorly water-soluble drug solubility through electrospun drug-loaded nanofibers].

作者信息

Yu Deng-Guang, Zhang Xiao-Fei, Shen Xia-Xia, Branford-White Chris, Zhu Li-Min

机构信息

College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, China.

出版信息

Yao Xue Xue Bao. 2009 Oct;44(10):1179-82.

Abstract

The improving effect of electrospun drug-loaded nanofibers on the solubility of poorly water-soluble drug was investigated in the present research. Drug-loaded nanofibers were successfully prepared using electrospinning process with helicid as the poorly water-soluble model drug and polyvinylpyrrolidone K60 (PVP K60) as the filament-forming matrix. Scanning electron microscopy observation demonstrated that the nanofibers had a three-dimensional continuous web structure, and had well smooth surface and a diameter between 400-600 nm. X-ray diffraction results suggested that helicid lost its original crystal structure but highly distributed into the nanofibers in an amorphous state, resulting from the hydrogen bonding interactions between the carboxylic group of PVP K60 and the hydroxyl groups of helicid. The drug-loaded nanofibers obviously improved helicid's solubility, and were able to completely release the whole drug in 60 s. Electrospun drug-loaded nanofibers can improve the solubility and release profiles of poorly water-soluble drug.

摘要

本研究考察了电纺载药纳米纤维对难溶性药物溶解度的改善作用。以难溶性模型药物豆腐果苷和聚乙烯吡咯烷酮K60(PVP K60)为成丝基质,采用静电纺丝工艺成功制备了载药纳米纤维。扫描电子显微镜观察表明,纳米纤维具有三维连续网状结构,表面光滑,直径在400 - 600 nm之间。X射线衍射结果表明,由于PVP K60的羧基与豆腐果苷的羟基之间存在氢键相互作用,豆腐果苷失去了原有的晶体结构,以无定形状态高度分散在纳米纤维中。载药纳米纤维显著提高了豆腐果苷的溶解度,且能在60 s内完全释放全部药物。电纺载药纳米纤维可改善难溶性药物的溶解度和释放特性。

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