Wiggers Helton José, Chevallier Pascale, Copes Francesco, Simch Fernanda Heloisa, da Silva Veloso Felipe, Genevro Giovana Maria, Mantovani Diego
Laboratory for Biomaterials and Bioengineering (LBB-BPK), Associação de Ensino, Pesquisa e Extensão BIOPARK, Toledo, Brazil.
Laboratory for Biomaterials and Bioengineering (LBB-UL), Canada Research Chair Tier I, Department of Min-Met-Materials Engineering and CHU de Quebec Research Center, Division Regenerative Medicine, Laval University, Quebec, Canada.
Front Bioeng Biotechnol. 2022 Mar 14;10:814162. doi: 10.3389/fbioe.2022.814162. eCollection 2022.
Natural polymer-based films, due to their favorable biological and mechanical properties, have demonstrated great potential as coatings for biomedical applications. Among them, chitosan films have been widely studied both as coating materials and as controlled drug release systems. Crosslinkers are often used to tune chitosan's crosslinking degree and thus to control the drug release kinetics. For this purpose, quercetin, a plant-derived natural polyphenol, has gained attention as a crosslinker, mainly for its intrinsic anti-inflammatory, antioxidant, and antibacterial features. In this study, chitosan films crosslinked with three different concentrations of quercetin (10, 20, and 30% w/w) have been used as controlled release systems for the delivery of the antibacterial drug trimethoprim (TMP, 10% w/w). Physicochemical and antimicrobial properties were investigated. Surface wettability and composition of the films were assessed by contact angle measurements, X-ray photoelectron spectroscopy (XPS), and Fourier-transform infrared spectroscopy (FTIR), respectively. The release kinetic of TMP in phosphate-buffered saline (PBS) and 2-(N-morpholino) ethanesulfonic acid (MES) was studied over time. Finally, antibacterial properties were assessed on and S. through Kirby-Bauer disc diffusion and micro-dilution broth assays. Results show that quercetin, at the tested concentrations, clearly increases the crosslinking degree in a dose-dependent manner, thus influencing the release kinetic of the loaded TMP while maintaining its bactericidal effects. In conclusion, this work demonstrates that quercetin-crosslinked chitosan films represent a promising strategy for the design of antibiotic-releasing coatings for biomedical applications.
基于天然聚合物的薄膜，因其良好的生物学和力学性能，在生物医学应用涂层方面展现出巨大潜力。其中，壳聚糖薄膜作为涂层材料和控释药物系统都得到了广泛研究。交联剂常被用于调节壳聚糖的交联度，从而控制药物释放动力学。为此，槲皮素，一种植物源天然多酚，作为交联剂受到关注，主要因其固有的抗炎、抗氧化和抗菌特性。在本研究中，用三种不同浓度（10%、20%和30% w/w）的槲皮素交联的壳聚糖薄膜被用作抗菌药物甲氧苄啶（TMP，10% w/w）的控释系统。对其物理化学和抗菌性能进行了研究。分别通过接触角测量、X射线光电子能谱（XPS）和傅里叶变换红外光谱（FTIR）评估了薄膜的表面润湿性和组成。研究了TMP在磷酸盐缓冲盐水（PBS）和2-（N-吗啉基）乙磺酸（MES）中的释放动力学随时间的变化。最后，通过 Kirby-Bauer 纸片扩散法和微量稀释肉汤法评估了对 和 的抗菌性能。结果表明，在所测试的浓度下，槲皮素以剂量依赖的方式显著提高了交联度，从而影响了负载的TMP的释放动力学，同时保持其杀菌效果。总之，这项工作表明槲皮素交联的壳聚糖薄膜是设计用于生物医学应用的抗生素释放涂层的一种有前景的策略。
