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用于多功能生物医学应用的新型载酒石酸溴莫尼定长效聚己内酯/聚乙烯吡咯烷酮纳米纤维:制备、表征及抗菌评估

Novel long-acting brimonidine tartrate loaded-PCL/PVP nanofibers for versatile biomedical applications: fabrication, characterization and antimicrobial evaluation.

作者信息

Salim Samar A, Badawi Noha M, El-Moslamy Shahira H, Kamoun Elbadawy A, Daihom Baher A

机构信息

Nanotechnology Research Center (NTRC), The British University in Egypt (BUE) Cairo 11837 Egypt

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, The British University in Egypt (BUE) Cairo 11837 Egypt.

出版信息

RSC Adv. 2023 May 16;13(22):14943-14957. doi: 10.1039/d3ra02244g. eCollection 2023 May 15.

DOI:10.1039/d3ra02244g
PMID:37200698
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10186146/
Abstract

The global state of antibiotic resistance highlights the necessity for new drugs that can treat a wide range of microbial infections. Drug repurposing has several advantages, including lower costs and improved safety compared to developing a new compound. The aim of the current study is to evaluate the repurposed antimicrobial activity of Brimonidine tartrate (BT), a well-known antiglaucoma drug, and to potentiate its antimicrobial effect by using electrospun nanofibrous scaffolds. BT-loaded nanofibers were fabricated in different drug concentrations (1.5, 3, 6, and 9%) the electrospinning technique using two biopolymers (PCL and PVP). Then, the prepared nanofibers were characterized by SEM, XRD, FTIR, swelling ratio, and drug release. Afterward, the antimicrobial activities of the prepared nanofibers were investigated using different methods against several human pathogens and compared to the free BT. The results showed that all nanofibers were prepared successfully with a smooth surface. The diameters of nanofibers were reduced after loading of BT compared to the unloaded ones. In addition, scaffolds showed controlled-drug release profiles that were maintained for more than 7 days. The antimicrobial assessments revealed good activities for all scaffolds against most of the investigated human pathogens, particularly the one prepared with 9% BT which showed superiority in the antimicrobial effect over other scaffolds. To conclude, our findings proved the capability of nanofibers in loading BT and improving its repurposed antimicrobial efficacy. Therefore, it could be a promising carrier for BT to be used in combating numerous human pathogens.

摘要

全球抗生素耐药状况凸显了研发可治疗多种微生物感染的新药的必要性。与开发新化合物相比,药物重新利用具有多种优势,包括成本更低和安全性更高。本研究的目的是评估著名的抗青光眼药物酒石酸溴莫尼定(BT)重新利用后的抗菌活性,并通过使用电纺纳米纤维支架增强其抗菌效果。采用两种生物聚合物(聚己内酯和聚乙烯吡咯烷酮),利用电纺丝技术制备了不同药物浓度(1.5%、3%、6%和9%)的负载BT的纳米纤维。然后,通过扫描电子显微镜、X射线衍射、傅里叶变换红外光谱、溶胀率和药物释放对制备的纳米纤维进行表征。之后,采用不同方法研究了制备的纳米纤维对几种人类病原体的抗菌活性,并与游离BT进行比较。结果表明,所有纳米纤维均成功制备,表面光滑。与未负载BT的纳米纤维相比,负载BT后纳米纤维的直径减小。此外,支架显示出可控的药物释放曲线,可维持7天以上。抗菌评估显示,所有支架对大多数研究的人类病原体均具有良好的活性,特别是用9% BT制备的支架,其抗菌效果优于其他支架。总之,我们的研究结果证明了纳米纤维负载BT的能力及其提高重新利用后的抗菌效果的能力。因此,它可能是BT用于对抗多种人类病原体的一种有前途的载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d47c/10186146/ef2f38e61805/d3ra02244g-f9.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d47c/10186146/a637db31d7a2/d3ra02244g-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d47c/10186146/ef2f38e61805/d3ra02244g-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d47c/10186146/a14b144c41b7/d3ra02244g-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d47c/10186146/24f39aa3c7d2/d3ra02244g-f2.jpg
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