Preparation of an optimized ciprofloxacin-loaded chitosan nanomicelle with enhanced antibacterial activity

Objective: The objective of this study was to evaluate the effect of lipid structure on physicochemical properties of chitosan-fatty acid nanomicelles and prepare an optimum ciprofloxacin-loaded formulation from these conjugates which could enhance the antibacterial effects of drug against some important pathogens like P. aeruginosa.

Significance: Nowadays, resistance in infectious diseases is a growing worldwide concern. Nanocarriers can increase the therapeutic index and consequently reduce the antibiotic resistance. By site-specific delivery of drug, the adverse effects of broad-spectrum antibiotics such as ciprofloxacin would be reduced.

Methods: Fatty acid grafted chitosan conjugates were synthetized in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The effects of fatty acid type (stearic acid, palmitic acid, and linoleic acid) on physicochemical properties of conjugates were investigated. Ciprofloxacin was encapsulated in nanomicelles by thin film hydration method. Also, the preparation process was optimized with a central composite design. The antibacterial effect of optimum formulation against P. aeruginosa, K. pneumoniae, and S. pneumoniae species was determined.

Results: All conjugates were synthetized with high yield values and the substitution degrees ranged between 2.13 and 35.46%. Ciprofloxacin was successfully encapsulated in nanomicelles. The optimum formulation showed high drug loading (≈?19%), with particle size of about 260?nm and a sustained release profile of ciprofloxacin. The minimum inhibitory concentrations of ciprofloxacin in optimum formulation against P. aeruginosa and K. pneumoniae species were 4 and 2 times lower in comparison with the free drug, respectively.

Conclusions: The antibacterial effect of ciprofloxacin was improved by encapsulation of drug in chitosan nanomicelles.     

Broad-Spectrum Bactericidal Activity of a Synthetic Random Copolymer Based on 2-Methoxy-6-(4-Vinylbenzyloxy)-Benzylammonium Hydrochloride

Low-molecular-weight organic ammonium salts exert excellent antimicrobial effects by interacting lethally with bacterial membranes. Unfortunately, short-term functionality and high toxicity limit their clinical application. On the contrary, the equivalent macromolecular ammonium salts, derived from the polymerization of monomeric ammonium salts, have demonstrated improved antibacterial potency, a lower tendency to develop resistance, higher stability, long-term activity, and reduced toxicity. A water-soluble non-quaternary copolymeric ammonium salt (P7) was herein synthetized by copolymerizing 2-methoxy-6-(4-vinylbenzyloxy)-benzylammonium hydrochloride monomer with N, N-di-methyl-acrylamide. The antibacterial activity of P7 was assessed against several multidrug-resistant (MDR) clinical isolates of both Gram-positive and Gram-negative species. Except for colistin-resistant Pseudomonas aeruginosa, most isolates were susceptible to P7, also including some Gram-negative bacteria with a modified charge in the external membrane. P7 showed remarkable antibacterial activity against isolates of Enterococcus, Staphylococcus, Acinetobacter, and Pseudomonas, and on different strains of Escherichia coli and Stenotrophomonas maltophylia, regardless of their antibiotic resistance. The lowest minimal inhibitory concentrations (MICs) observed were 0.6–1.2 µM and the minimal bactericidal concentrations (MBC) were frequently overlapping with the MICs. In 24-h time–kill and turbidimetric studies, P7 displayed a rapid non-lytic bactericidal activity. P7 could therefore represent a novel and potent tool capable of counteracting infections sustained by several bacteria that are resistant to the presently available antibiotics.     

MIC薄膜多晶硅材料的动态镍吸除技术基本机理及其应用

首先阐述了MIC薄膜多晶硅材料动态镍吸杂技术的基本机理和主要工艺过程,然后以多晶硅薄膜晶体管(poly-Si TFT)为例研究了动态吸杂技术的应用.在研究金属诱导晶化多晶硅材料(MIC poly-Si)和以之为有源层的poly-Si TFT的过程中,发现在MIC多晶硅薄膜中含有部分残余的镍成份.而大部分存在于对撞晶界的残余镍成份会造成大量的缺陷,这将导致TFT器件性能乃至整个系统的稳定性和可靠性的降低.为了改善MIC薄膜及器件质量,我们采用磷硅玻璃(PSG)动态镍吸杂技术,有效地吸除镍,降低多晶硅中镍的残留量,改善对撞晶界的缺陷密度,降低用之制备TFT的漏电流.该技术工艺过程简单,处理成本低,适合于大批量的工业化生产,有望成为制备高稳定性微电子器件与电路系统的必需工艺技术.     

X65管线钢在成品油管道沉积物中的微生物腐蚀行为

目的分析华南一成品油管道内微生物腐蚀(MIC)的主要原因及行为,为成品油管道安全运行提供支撑。方法利用微生物分析、表面分析和电化学手段,分析成品油管道沉积物中可能引发腐蚀的细菌群落,研究细菌群落协同作用下,X65管线钢的腐蚀状态,并对X65管线钢在成品油管道沉积物稀释液中的MIC行为进行分析。结果从属水平来看,成品油管道沉积物中相对丰度大于0.1%的29种菌属中有13种可能引发MIC。在实验的1～3天,天然稀释液体系(X65-Bacteria)的OCP持续正移,且正移幅度大于灭菌稀释液体系(X65-Asepsis),第3天的EIS阻抗弧半径最大。在实验的3～7天,天然稀释液(X65-Bacterias)体系的OCP负移,且负移程度明显大于灭菌稀释液(X65-Asepsis)体系。在实验的第7天,天然稀释液(X65-Bacterias)体系的阻抗弧半径小于灭菌稀释液(X65-Asepsis)体系,且自腐蚀电位更负。对生成的生物膜进行成分分析发现,生物膜和腐蚀产物膜主要由有机物和铁的氧化物组成。结论柠檬酸杆菌属(Citrobacter)和鞘氨醇单胞菌属(Sphingomonas)可能是造成华南一成品油管道沉积物中MIC的主要菌群。在管道沉积物中细菌群落的协同作用下,X65管线钢的腐蚀速度加快。     

车辆牌照分割方法

提出了一种快速准确车辆牌照的分割方法。首先利用形态学算子获取车牌的候选区域,剔除较小的和较大的区域;对保留的候选区域利用Trajkovic算法获取角点;最后对检测后的结果聚类,从而分割出包含车牌区域的子图像。实验证明,该方法效果好,分割速度快。     

苦瓜总皂甙最小抑菌浓度和最佳抑菌条件的研究

苦瓜总皂甙是苦瓜中有效成分,具有抑菌等作用。通过绘制生长曲线判断苦瓜总皂甙对大肠杆菌、金黄色葡萄球菌、枯草芽孢杆菌和黑曲霉菌生长曲线的影响。采用琼脂稀释法测定苦瓜总皂甙的最小抑菌浓度(MIC)。运用正交实验设计法确定苦瓜总皂甙的最佳抑菌条件。结果表明,苦瓜总皂甙对黑曲霉菌的生长几乎没有抑菌作用。浓度为50、100、150、200mg/mL的苦瓜总皂甙对大肠杆菌、枯草芽孢杆菌、金黄色葡萄球菌生长均有抑制作用,且以150mg/mL浓度时为最强,MIC分别为30、40、30mg/mL。苦瓜总皂甙对大肠杆菌和金黄色葡萄球菌的最佳抑菌条件为:40℃下,pH为6.0时,抑菌20h。     

黄芪提取物对细菌抑制作用的研究

本文以黄芪作为研究对象,利用制得的黄芪提取物对多种细菌进行了抑菌活性实验,结果表明:黄芪提取物抑菌作用因菌种不同而最低抑菌浓度有所不同,大肠杆菌为7.5%、产气杆菌为8%、变形杆菌为4.5%、金黄色葡萄球菌为9.5%、沙门氏菌10%,其抑菌直径分别为:大肠杆菌8.6mm、产气杆菌8.1mm、变形杆菌8.2mm、金黄色葡萄球菌7.7mm、沙门氏菌8.4mm,表明对常见细菌有较好的抑制作用,其抑菌效果与时间有一定关系,在121℃湿热条件下20min后黄芪提取物抑菌效果基本不变,说明制得的黄芪提取物具有良好的热稳定性。此外,黄芪提取物抑菌浓度与时间有关。     

无花果叶提取物的抑菌作用研究

为探讨无花果叶逐级提取物的抑菌作用,实验测定了无花果叶逐级提取物对各实验菌种的抑菌圈及最低抑菌浓度,结果表明各级提取物对实验菌分别有不同程度的抑菌作用,其中对金黄色葡萄球菌和枯草杆菌的抑菌作用最为明显,各级提取物的抑菌强度依次为:乙酸乙酯萃取物(金黄色葡萄球菌:MIC≤6.25mg/mL,枯草杆菌MIC:≤12.5mg/mL)、正丁醇萃取液(两种菌的抑菌作用:MIC≤25mg/mL)、石油醚萃取液(两种菌的抑菌作用:MIC≤50mg/mL),其中乙酸乙酯萃取物的抑菌活性最强。     

Inhibitory effects of 4-chlorosalicylic acid on mushroom tyrosinase and its antimicrobial activities

The inhibitory effects of 4-chlorosalicylic acid on the activity of mushroom tyrosinase have been investigated. The results showed that 4-chlorosalicylic acid could strongly inhibit both monophenolase activity and diphenolase activity. The IC₅₀ values were estimated as 1.89 mM and 1.10 mM for monophenolase and diphenolase activities, respectively. For the monophenolase activity, 4-chlorosalicylic acid could not only lengthen the lag time, but also decrease the steady-state rate. For the diphenolase activity, kinetic analyses showed that the inhibition by 4-chlorosalicylic acid was reversible and its mechanism was mixed-II type, which is different from salicylic acid. The inhibition constants (K_I and K_IS) were determined to be 1.51 mM and 0.82 mM, respectively. Furthermore, the antibacterial activity against Escherichia coli, Bacillus subtilis and Staphyloccocus aureus and antifungal activity against Aspergillus niger and Candida boidinii were investigated. The results showed that 4-chlorosalicylic acid was the most effective against E. coli with the MIC of 250 μg/ml and with the MBC of 500 μg/ml.     

硫酸盐还原菌微生物腐蚀研究进展

本文简单介绍了硫酸盐还原菌(SRB)引起的微生物腐蚀(MIC)的各种机理、环境因素引起的SRB的生长与变异及SRB腐蚀防控措施的研究进展。