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

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%) via the electrospinning technique using two biopolymers (PCL and PVP). Then, the prepared nanofibers were characterized by SEM, XRD, FTIR, swelling ratio, and in vitro drug release. Afterward, the antimicrobial activities of the prepared nanofibers were investigated in vitro 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 in vitro 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.

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Materials

Polycaprolactone (PCL, Mwt 14 KDa) was purchased from Sigma-Aldrich, Japan, and polyvinyl pyrrolidone (PVP, Mwt 40 KDa) was bought from Thermo-Fisher, Germany. Dichloromethane (DCM purity ≥ 99%) and methanol (90%) were obtained from Fisher Scientific, UK. Orchidia Pharmaceutical Co. in Egypt kindly supplied Brimonidine tartrate (BT). The human pathogens that were employed in this work were Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia, Staphylococcus aureus, Staphylococcus epidermidis, Bacillus cereus, Candida albicans, Candida tropicals, and Candida glabrata were collected from Bioprocess Development Department, GEBRI, SRTA-City Alexandria, Egypt.

Samar A. Salim, Noha M. Badawi, Shahira H. EL-Moslamy, Elbadawy A. Kamoun and Baher A. Daihom, Novel long-acting brimonidine tartrate loaded-PCL/PVP nanofibers for versatile biomedical applications, fabrication, characterization and antimicrobial evaluation, Issue 22, 2023, Issue in Progress, Article type Paper, Submitted04 Apr 2023, Accepted08 May 2023, First published16 May 2023, DOI https://doi.org/10.1039/D3RA02244G