Le Hung, Dé Emmanuelle, Le Cerf Didier, Karakasyan Carole
Sciences & Technic Faculty, Univ Rouen Normandie, INSA Rouen Normandie, CNRS, PBS UMR 6270, 76000 Rouen, France.
Antibiotics (Basel). 2023 Jun 16;12(6):1066. doi: 10.3390/antibiotics12061066.
The poor bioavailability of antibiotics at infection sites is one of the leading causes of treatment failure and increased bacterial resistance. Therefore, developing novel, non-conventional antibiotic delivery strategies to deal with bacterial pathogens is essential. Here, we investigated the encapsulation of two fluoroquinolones, ciprofloxacin and levofloxacin, into polymer-based nano-carriers (nano-antibiotics), with the goal of increasing their local bioavailability at bacterial infection sites. The formulations were optimized to achieve maximal drug loading. The surfaces of nano-antibiotics were modified with anti-staphylococcal antibodies as ligand molecules to target pathogens. The interaction of nano-antibiotics with the bacterial cells was investigated via fluorescent confocal microscopy. Conventional tests (MIC and MBC) were used to examine the antibacterial properties of nano-antibiotic formulations. Simultaneously, a bioluminescence assay model was employed, revealing the rapid and efficient assessment of the antibacterial potency of colloidal systems. In comparison to the free-form antibiotic, the targeted nano-antibiotic exhibited enhanced antimicrobial activity against both the planktonic and biofilm forms of . Furthermore, our data suggested that the efficacy of a targeted nano-antibiotic treatment can be influenced by its antibiotic release profile.
抗生素在感染部位的生物利用度低是治疗失败和细菌耐药性增加的主要原因之一。因此,开发新型的、非常规的抗生素递送策略来应对细菌病原体至关重要。在此,我们研究了将两种氟喹诺酮类药物环丙沙星和左氧氟沙星封装到基于聚合物的纳米载体(纳米抗生素)中,目的是提高它们在细菌感染部位的局部生物利用度。对制剂进行了优化以实现最大载药量。用抗葡萄球菌抗体作为配体分子修饰纳米抗生素的表面,以靶向病原体。通过荧光共聚焦显微镜研究了纳米抗生素与细菌细胞的相互作用。使用常规测试(MIC和MBC)来检测纳米抗生素制剂的抗菌性能。同时,采用生物发光测定模型,揭示了对胶体系统抗菌效力的快速有效评估。与游离形式的抗生素相比,靶向纳米抗生素对浮游菌和生物膜形式的[此处原文缺失具体细菌名称]均表现出增强的抗菌活性。此外,我们的数据表明,靶向纳米抗生素治疗的疗效可能受其抗生素释放曲线的影响。