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地拉氟沙星包覆金纳米颗粒(DFX-AuNPs):一种有效的氟喹诺酮类抗生素抗菌纳米制剂。

Delafloxacin-Capped Gold Nanoparticles (DFX-AuNPs): An Effective Antibacterial Nano-Formulation of Fluoroquinolone Antibiotic.

作者信息

Abu Lila Amr Selim, Huwaimel Bader, Alobaida Ahmed, Hussain Talib, Rafi Zeeshan, Mehmood Khalid, Abdallah Marwa H, Hagbani Turki Al, Rizvi Syed Mohd Danish, Moin Afrasim, Ahmed Abobakr F

机构信息

Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Ha'il 81442, Saudi Arabia.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.

出版信息

Materials (Basel). 2022 Aug 18;15(16):5709. doi: 10.3390/ma15165709.

Abstract

New antibiotics are seen as 'drugs of last resort' against virulent bacteria. However, development of resistance towards new antibiotics with time is a universal fact. Delafloxacin (DFX) is a new fluoroquinolone antibiotic that differs from existing fluoroquinolones by the lack of a protonatable substituent, which gives the molecule a weakly acidic nature, affording it higher antibacterial activity under an acidic environment. Furthermore, antibiotic-functionalized metallic nanoparticles have been recently emerged as a feasible platform for conquering bacterial resistance. In the present study, therefore, we aimed at preparing DFX-gold nano-formulations to increase the antibacterial potential of DFX. To synthesize DFX-capped gold nanoparticles (DFX-AuNPs), DFX was used as a reducing and stabilizing/encapsulating agent. Various analytical techniques such as UV-visible spectroscopy, TEM, DLS, FTIR and zeta potential analysis were applied to determine the properties of the synthesized DFX-AuNPs. The synthesized DFX-AuNPs revealed a distinct surface plasmon resonance (SPR) band at 530 nm and an average size of 16 nm as manifested by TEM analysis. In addition, Zeta potential results (-19 mV) confirmed the stability of the synthesized DFX-AuNPs. Furthermore, FTIR analysis demonstrated that DFX was adsorbed onto the surface of AuNPs via strong interaction between AuNPs and DFX. Most importantly, comparative antibacterial analysis of DFX alone and DFX-AuNPs against Gram-negative ( and ) and Gram-positive ( and ) verified the superior antibacterial activity of DFX-AuNPs against the tested microorganisms. To sum up, DFX gold nano-formulations can offer a promising possible solution, even at a lower antibiotic dose, to combat pathogenic bacteria.

摘要

新型抗生素被视为对抗毒性细菌的“最后一道防线”。然而,随着时间的推移,细菌对新型抗生素产生耐药性是一个普遍存在的事实。德拉沙星(DFX)是一种新型氟喹诺酮类抗生素,它与现有的氟喹诺酮类药物不同之处在于缺乏可质子化取代基,这使得该分子具有弱酸性,在酸性环境下具有更高的抗菌活性。此外,抗生素功能化金属纳米颗粒最近已成为克服细菌耐药性的一个可行平台。因此,在本研究中,我们旨在制备DFX-金纳米制剂以提高DFX的抗菌潜力。为了合成DFX包覆的金纳米颗粒(DFX-AuNPs),DFX被用作还原剂和稳定/包封剂。采用紫外可见光谱、透射电子显微镜(TEM)、动态光散射(DLS)、傅里叶变换红外光谱(FTIR)和zeta电位分析等多种分析技术来测定合成的DFX-AuNPs的性质。合成的DFX-AuNPs在530 nm处显示出明显的表面等离子体共振(SPR)带,TEM分析表明其平均粒径为16 nm。此外,zeta电位结果(-19 mV)证实了合成的DFX-AuNPs的稳定性。此外,FTIR分析表明,DFX通过AuNPs与DFX之间的强相互作用吸附在AuNPs表面。最重要的是,单独的DFX和DFX-AuNPs对革兰氏阴性菌( 和 )和革兰氏阳性菌( 和 )的比较抗菌分析证实了DFX-AuNPs对受试微生物具有更强的抗菌活性。综上所述,即使在较低的抗生素剂量下,DFX金纳米制剂也可能为对抗病原菌提供一个有前景的解决方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd24/9415438/b16c947f60b5/materials-15-05709-g001.jpg

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