载吲哚美辛纳米纤维的制备及其促伤口愈合性能  

Preparation and Wound Healing Properties of Indomethacin-Loaded Nanofibers

作　　者：何香 王晶 邢梓鑫 刘哲鹏[1] 王淑仪 聂丽蓉 HE Xiang;WANG Jing;XING Zi-Xin;LIU Zhe-Peng;WANG Shu-Yi;NIE Li-Rong(School of Health Science and Engineering,University of Shanghai for Science and Technology,Shanghai 200093,China)

机构地区：[1]上海理工大学健康科学与工程学院,上海200093

出　　处：《应用化学》2024年第11期1629-1638,共10页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金面上项目(No.32372307)资助。

摘　　要：吲哚美辛是一种非甾体抗炎药,具有解热镇痛和消炎等药理作用。然而,吲哚美辛的低水溶性、低生物利用率及其对胃肠道的刺激,严重制约了其在临床上的应用。针对上述问题,以尤特奇RS100、聚乙烯吡咯烷酮(PVP K30)为缓释基质,利用静电纺丝技术,制备了一种具有双相释放药物性能的载吲哚美辛核壳结构纳米纤维。通过正交设计实验优化的制备工艺参数为电压16.94 kV,接收距离11.02 cm,流速1.44 mL/h。该载药纳米纤维直径多分布于600~800 nm间,平均直径为(675±177)nm,形貌良好,呈现同轴结构,有利于吲哚美辛的双相释放。体外释放及初步药效学研究表明该载药纳米纤维能够持续释放25 h,仅需不到2 h即可释放出累计释放量的50%,具有速释、缓释双相释药性能,抗炎镇痛作用优良,能够有效促进伤口愈合。期望本研究能够为医用新型创伤敷料的发展提供参考。Indomethacin is a nonsteroidal anti-inflammatory drug with pharmacologic effects such as antipyretic and analgesic and anti-inflammatory.However,indomethacin's low water solubility,low bioavailability and its irritation to the gastrointestinal tract have severely limited its clinical application.To address these problems,an indomethacin-loaded core-shell structured nanofiber with biphasic drug release properties was prepared by electrostatic spinning using Eutectic RS100 and polyvinylpyrrolidone(PVP K30)as a slow-release matrix.The parameters of the preparation process optimized by orthogonal design test were voltage 16.94 kV,receiver distance 11.02 cm and flow rate 1.44 mL/h.The diameter of the drug-loaded nanofibers was mostly distributed between 600~800 nm,with an average diameter of(675±177)nm,which had good morphology and coaxial structure,which was conducive to the biphasic release of indomethacin.In vitro release and preliminary pharmacodynamic studies have shown that the drug-loaded nanofibers can be continuously released for about 25 h,and release 50%of the cumulative release in less than 2 h,which has the performance of immediate-release and sustained-release biphasic release,excellent anti-inflammatory and analgesic effects,and can effectively promote wound healing.It is expected that this study can provide a reference for the development of new medical wound dressings.

关 键 词：静电纺丝 吲哚美辛 缓释系统 创伤敷料 双相释药 

分 类 号：O636[理学—高分子化学]