Abstract：
The study aimed to improve the treatment of impetigo with naturally occurring quercetin and its copper-quercetin (Cu-Q) complex by preparing sustained-release (SR) nanoparticles of polycaprolactone (PCL). The solvent evaporation method was used for the copper-quercetin (Cu-Q) complex formation, and their PCL nanoparticles (PCL-NPs, Q-PCL-NPs, and Cu-Q-PCL-NPs) were prepared by the high-pressure homogenization method. Synthesis of nanoparticles was confirmed by their physicochemical and antibacterial properties of quercetin against Gram-positive as well as Gram-negative bacteria. The percentage loading efficiency of quercetin and release in 100 mM of phosphate buffer pH 7.4 and 5.5 at 37 °C was found to be more than 90% after 24 h with the zero-order release pattern. Minimum inhibitory concentration of nanoparticles was found to increase threefold in the case of Cu-Q-PCL-NPs may be due to the synergistic antibacterial behavior. Scanning electron microscopy showed spherical nanoparticles, and surface roughness was confirmed by atomic force microscopy analysis. Fortunately, no sign of irritation on rat skin even at 3%, was seen. In vitro antioxidant assay by 2,2-diphenyl-1-picrylhydrazyl reduction was found to be ≤80 ± 0.02% which confirmed their scavenging activity. Interestingly, for the ex vivo study, the tape-stripping model was applied against Staphylococcus aureus containing rats and showed the formation of the epidermal layer within 4-5 days. Confirmation of antibacterial activity of pure quercetin, from Cu-Q complex, and their SR release from Q-PCL-NPs and Cu-Q-PCL-NPs was considered an effective tool for the treatment of skin diseases and can be used as an alternative of already resistant ciprofloxacin in impetigo.
摘要：
该研究旨在通过制备聚己内酯（PCL）的缓释（SR）纳米颗粒来改善天然槲皮素及其铜-槲皮素（Cu-Q）复合物对脓疱病的治疗。溶剂蒸发法用于铜-槲皮素(Cu-Q)络合物的形成,和它们的PCL纳米颗粒(PCL-NP，Q-PCL-NP,和Cu-Q-PCL-NPs）通过高压均质法制备。通过槲皮素对革兰氏阳性细菌和革兰氏阴性细菌的物理化学和抗菌性质证实了纳米颗粒的合成。在零级释放模式下，发现槲皮素的百分比加载效率和在37°C下100mM磷酸盐缓冲液pH7.4和5.5中的释放在24小时后超过90％。在Cu-Q-PCL-NP的情况下，发现纳米颗粒的最小抑制浓度增加了三倍，这可能是由于协同抗菌行为。扫描电子显微镜显示球形纳米颗粒，表面粗糙度由原子力显微镜分析证实。幸运的是,即使在3%时，对大鼠皮肤也没有刺激的迹象，被看见了。通过2,2-二苯基-1-吡啶酰肼还原的体外抗氧化剂测定发现≤80±0.02％，这证实了它们的清除活性。有趣的是,对于离体研究，胶带剥离模型应用于含金黄色葡萄球菌的大鼠，并显示在4-5天内形成表皮层。确认纯槲皮素的抗菌活性，来自Cu-Q络合物，它们从Q-PCL-NP和Cu-Q-PCL-NP中释放的SR被认为是治疗皮肤病的有效工具，可以用作已经耐药的环丙沙星的替代品。
