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用于口腔念珠菌病治疗的速溶克霉唑复合PVP/HPβCD纳米纤维

Fast-acting clotrimazole composited PVP/HPβCD nanofibers for oral candidiasis application.

作者信息

Tonglairoum Prasopchai, Ngawhirunpat Tanasait, Rojanarata Theerasak, Kaomongkolgit Ruchadaporn, Opanasopit Praneet

机构信息

Pharmaceutical Development of Green Innovations Group (PDGIG) Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand.

出版信息

Pharm Res. 2014 Aug;31(8):1893-906. doi: 10.1007/s11095-013-1291-1. Epub 2014 Feb 20.

Abstract

PURPOSE

This study investigates fabrication of clotrimazole (CZ)-composited electrospun Polyvinylpyrrolidone/Hydroxypropyl-β-cyclodextrin (PVP/HPβCD) blended nanofiber mats for oral candidiasis applications.

METHODS

PVP/HPβCD blended nanofiber mats containing clotrimazole were electrospun and characterized using SEM, DSC and XRPD. The solvent system ethanol: water: benzyl alcohol (EtOH:H2O:BzOH) with a 70:20:10 ratio was optimal for the electrospinning process. Various amounts of CZ were loaded into the nanofiber mats. The nanofiber mats was further investigated for drug release, antifungal activity and cytotoxicity.

RESULTS

The fiber diameters in the mats were in the nanometer range. The DSC and XRPD revealed a molecular dispersion of amorphous CZ in the nanofiber mats. The loading capacity increased when CZ content was raised. A fast dissolved and released of CZ from the nanofibers mat was achieved. The ability of the CZ-loaded nanofiber mats to kill the Candida depended on the amount of CZ in the mats; moreover, the CZ-loaded nanofibers killed the Candida significantly faster than the CZ powder and lozenges with low cytotoxicity.

CONCLUSIONS

CZ-loaded nanofiber mats were successfully electrospun. They exhibited rapid antifungal activity in vitro relative to CZ powder and lozenges. Further in vivo studies are needed to investigate for their application in oral candidiasis.

摘要

目的

本研究旨在制备用于口腔念珠菌病的含克霉唑(CZ)的电纺聚乙烯吡咯烷酮/羟丙基-β-环糊精(PVP/HPβCD)共混纳米纤维垫。

方法

电纺含克霉唑的PVP/HPβCD共混纳米纤维垫,并通过扫描电子显微镜(SEM)、差示扫描量热法(DSC)和X射线粉末衍射(XRPD)进行表征。乙醇:水:苯甲醇(EtOH:H₂O:BzOH)比例为70:20:10的溶剂体系对电纺过程最为适宜。向纳米纤维垫中加入不同量的CZ。进一步研究纳米纤维垫的药物释放、抗真菌活性和细胞毒性。

结果

垫中的纤维直径处于纳米范围。DSC和XRPD显示无定形CZ在纳米纤维垫中呈分子分散状态。随着CZ含量的增加,载药量提高。实现了CZ从纳米纤维垫中的快速溶解和释放。载CZ纳米纤维垫杀灭念珠菌的能力取决于垫中CZ的量;此外,载CZ纳米纤维杀灭念珠菌的速度明显快于CZ粉末和含片,且细胞毒性较低。

结论

成功电纺了载CZ纳米纤维垫。相对于CZ粉末和含片,它们在体外表现出快速的抗真菌活性。需要进一步进行体内研究以考察其在口腔念珠菌病中的应用。

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