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基于静电纺丝的玉米醇溶蛋白/聚(甲基丙烯酸二甲氨基乙酯)纳米纤维的双药物传递系统,用于同时递送双氯芬酸和泮托拉唑。

Electrospun zein/eudragit nanofibers based dual drug delivery system for the simultaneous delivery of aceclofenac and pantoprazole.

机构信息

Biomaterials Division, CSIR - Central Leather Research Institute, Chennai, India.

出版信息

Int J Pharm. 2012 Nov 15;438(1-2):117-22. doi: 10.1016/j.ijpharm.2012.07.075. Epub 2012 Aug 31.

DOI:10.1016/j.ijpharm.2012.07.075
PMID:22960320
Abstract

Electrospun composite zein/eudragit nanofibers were developed with an aim to deliver two different classes of drugs simultaneously that would restrict/compensate the adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs). Co-administration of proton pump inhibitors is beneficial for patients consuming NSAIDs for treating chronic ailments like arthritis. In this study, aceclofenac/pantoprazole loaded zein/eudragit S 100 nanofibers were developed using a single nozzle electrospinning process. The morphological analysis revealed the uniform and smooth surface of the drug loaded nanofibers. The physico-thermal characterization of nanofibers depicted the molecular integration of the drugs with the polymers and also confirmed that the drugs were evenly distributed in the nanofibers in an amorphous state. In vitro release studies ensure the efficiency of the developed fibers in sustaining the release of both the drugs up to 8h. In vivo animal experiments further confirmed that the co-administration of pantoprazole along with aceclofenac reduced the gastro-intestinal toxicity induced by NSAIDs. The histological evaluation revealed the preserved mucosal architecture of rat gastric tissue treated with drug loaded composite nanofibers. Thus, dual drug delivery system comprising polymers with different release characteristics has been successfully developed and further, oral delivery of aceclofenac with reduced side effects was achieved.

摘要

静电纺丝复合玉米醇溶蛋白/聚维酮纳米纤维的开发目的是同时输送两类药物,以限制/补偿非甾体抗炎药(NSAIDs)的不良反应。质子泵抑制剂的联合使用有利于接受 NSAIDs 治疗关节炎等慢性疾病的患者。在这项研究中,使用单喷嘴静电纺丝工艺开发了载有 aceclofenac/泮托拉唑的玉米醇溶蛋白/聚维酮 S100 纳米纤维。形态分析显示载药纳米纤维具有均匀光滑的表面。纳米纤维的物理热特性表明药物与聚合物的分子整合,并证实药物以无定形状态均匀分布在纳米纤维中。体外释放研究确保了所开发纤维在维持两种药物长达 8 小时的释放效率。体内动物实验进一步证实,泮托拉唑与 aceclofenac 的联合使用降低了 NSAIDs 引起的胃肠毒性。组织学评价显示,用载药复合纳米纤维处理的大鼠胃组织保留了粘膜结构。因此,成功开发了具有不同释放特性的聚合物的双药物传递系统,并进一步实现了 aceclofenac 的口服递送和减少副作用。

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