Mucoadhesive liposomes as ocular delivery system: physical,microbiological, and in vivo assessment

Background: Mucoadhesive drug delivery is a promising strategy to overcome ocular biopharmaceutical constraints. Objective and methods: Ciprofloxacin HCl-loaded reverse phase evaporation liposomes were coated with different concentrations and molecular weights of mucoadhesive biocompatible chitosan polymer to form chitosomes. This colloidal mucoadhesive system was evaluated in vitro and in vivo with respect to deliver the antibiotic to ocular surface. Results and conclusion: The results obtained pointed out that liposome coating process resulted in entrapment efficiency reduction and higher chitosan concentration, and molecular weight showed a more pronounced effect. No morphological differences between coated and uncoated liposomes were observed. Diffusion was the drug release mechanism from chitosomes. Concerning rheological behavior, pseudoplastic flow was characteristic to the prepared chitosomal dispersions. In addition, chitosan coating improved the ocular permeation of ciprofloxacin HCl. Microbiologically; this formulated system enhanced antimicrobial activity of ciprofloxacin HCl against both Gram-positive and Gram-negative bacteria. Moreover, this mucoadhesive system was able to inhibit the growth of Pseudomonas aeruginosa in rabbits' eyes for 24 hours when compared to the marketed preparation. In vivo bacterial conjunctivitis model elucidated that symptoms were controlled by the prolonged release formulation such as that done by the marketed product.     

Synthesis of Vegetable Fat Containing Chitosan Microparticles with Improved Physical and Delivery Properties

The present study describes the encapsulation of vegetable fats (cocoa butter and mango butter) within chitosan microparticles by double emulsion technique to prevent leaching of the internal apolar phase. Leaching studies suggested negligible leaching of the internal phase (～12–14%) when the fats were encapsulated as compared to the control (～40%). Fourier transform infrared spectroscopy and differential scanning calorimeter studies confirmed the successful encapsulation of fats. The release of drug (ciprofloxacin) from the microparticles was diffusion and erosion mediated and were capable to elicit antimicrobial activity against Escherichia coli. The study suggests that the developed microparticles have the potential for controlled delivery of antimicrobials.     

同时检测恩诺沙星和环丙沙星单克隆抗体的制备

为了产生同时检测恩诺沙星和环丙沙星的抗体,本研究采用戊二醛法制备突出恩诺沙星和环丙沙星共同结构的人工抗原。免疫Balb/c 小鼠的结果显示：使用糖基化载体所制备的免疫抗原,能够大幅提高所产生特异性抗体的滴度。通过细胞融合,筛选出一株对恩诺沙星和环丙沙星IC50 值分别为9.6ng/mL 和10.2ng/mL 的单克隆抗体。     

Antimicrobial Resistance and Whole-Genome Characterisation of High-Level Ciprofloxacin-Resistant Salmonella Enterica Serovar Kentucky ST 198 Strains Isolated from Human in Poland

Background: Salmonella Kentucky belongs to zoonotic serotypes that demonstrate that the high antimicrobial resistance and multidrug resistance (including fluoroquinolones) is an emerging problem. To the best of our knowledge, clinical S. Kentucky strains isolated in Poland remain undescribed. Methods: Eighteen clinical S. Kentucky strains collected in the years 2018–2019 in Poland were investigated. All the strains were tested for susceptibility to 11 antimicrobials using the disc diffusion and E-test methods. Whole genome sequences were analysed for antimicrobial resistance genes, mutations, the presence and structure of SGI1-K (Salmonella Genomic Island and the genetic relationship of the isolates. Results: Sixteen of 18 isolates (88.9%) were assigned as ST198 and were found to be high-level resistant to ampicillin (>256 mg/L) and quinolones (nalidixic acid MIC ≥ 1024 mg/L, ciprofloxacin MIC range 6–16 mg/L). All the 16 strains revealed three mutations in QRDR of GyrA and ParC. The substitutions of Ser83 → Phe and Asp87 → Tyr of the GyrA subunit and Ser80→Ile of the ParC subunit were the most common. One S. Kentucky isolate had qnrS1 in addition to the QRDR mutations. Five of the ST198 strains, grouped in cluster A, had multiple resistant determinants like blaTEM1-B, aac(6′)-Iaa, sul1 or tetA, mostly in SGI1 K. Seven strains, grouped in cluster B, had shorter SGI1-K with deletions of many regions and with few resistance genes detected. Conclusion: The results of this study demonstrated that a significant part of S. Kentucky isolates from humans in Poland belonged to ST198 and were high-level resistant to ampicillin and quinolones.     

壳聚糖微球对环丙沙星吸附的研究

采用分光光度法研究了功能高分子壳聚糖及其微球对环丙沙星的吸附及控制释放;考察了吸附时间、初始浓度及pH值对吸附的影响。     

Dyeing of wool with antibiotics to develop novel infection resistance materials for extracorporeal end use

Two antibiotics, doxycycline (Doxy) and ciprofloxacin (Cipro), were applied under a variety of conditions to wool and to hydrolyzed wool at 40°C. Nylon was used as a synthetic control. Sorption of Doxy was much higher in wool than in nylon, whereas sorption of Cipro was similar in both fibers. FTIR spectroscopy confirmed that a drastic increase in sorption of antibiotics by hydrolyzed wool was attributed to an increase in polar functional groups by peptide scission and in oxidized sulfur groups by cystine oxidation. Both sorption and zone of inhibition (ZOI) values were improved by hydrolysis of wool. Wool hydrolyzed for 20 or 40 min at 40°C and dyed with Doxy at 45°C for 3.5 h maintained around 30 mm of ZOI after 24 h of challenge by a simulated flow of blood. Wool hydrolyzed for 60 min at 40°C and dyed with Cipro at 45°C for 3.5 h also maintained its antibiotic activity for an extended time. For the most part, ZOI values for nylon dyed by both antibiotics were zero within 24 h. This technique produced infection‐resistant biomaterials of potential use in extra‐corporeal biomedical and biological applications. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 92: 3343–3354, 2004     

环丙沙星降解菌的筛选及其降解特性探究

为获取一株有效降解环丙沙星的菌株,并探究其在降解过程中的降解特性,利用高效液相色谱法筛选环丙沙星降解菌,根据菌落形态、生理生化特性以及16S rDNA基因序列分析,对降解菌进行鉴定;并研究菌株活性、胞内外物质以及细胞壁对质量浓度为4 μg/mL环丙沙星的降解作用。结果表明,罗伊氏乳杆菌WQ-Y1在物理吸附和生物降解的共同作用下,降解率最高可达70.2%,其胞内物质、胞外物质以及细胞壁对环丙沙星的降解率分别为17.7%、23.4%和37.0%,远低于活菌的降解率。可见罗伊氏乳杆菌WQ-Y1对环丙沙星的物理吸附作用和菌株体内的酶都并非是菌株降解环丙沙星的单一途径,而是依赖于完整的菌株活性。     

Controlled synthesis of Ag2O/g-C3N4 heterostructures using soft and hard templates for efficient and enhanced visible-light degradation of ciprofloxacin

Pluronic 31R1 surfactant and MCM-41 silica were used to fabricate mesoporous Ag₂O/g-C₃N₄ heterostructures with improved surface areas. The fabricated mesoporous nanocomposite was used to photo oxidize ciprofloxacin. The TEM images of Ag₂O/g-C₃N₄ indicated a uniform dispersion of spherical approximately 4-nm Ag₂O nanoparticles on g-C₃N₄. The mesoporous 0.9% Ag₂O@g-C₃N₄ heterostructure exhibited 100% efficiency in ciprofloxacin oxidation within 60 min when compared with the 25% efficiency in 120 min of pure mesoporous Ag₂O and 10% efficiency in 120 min of pure g-C₃N₄. The highest ciprofloxacin oxidation efficiency achieved was 100%, which was four and ten times better than those of Ag₂O and g-C₃N₄, respectively. This superior performance of the mesoporous Ag₂O/g-C₃N₄ was attributed to the high dispersion of nano-sized mesoporous Ag₂O particles on the g-C₃N₄ surface, narrow bandgap, and significantly high surface areas. The powerful interaction between Ag₂O and g-C₃N₄ ensured robust durability of Ag₂O/g-C₃N₄ heterostructures, which is evident in the fact that five recycling trials of the photocatalyst rendered a minimal loss of efficiency.     

环丙沙星-磷钼多金属氧酸盐的制备及热分解动力学

报道了环丙沙星与十二磷钼酸的多金属氧酸盐化合物,用元素分析、IR、TG-DTA等方法对其进行了表征,结果显示该化合物仍保持Keggin型结构特征。同时,采用TG-DTG技术研究了标题化合物在氮气气氛中的热分解机理及非等温动力学,它的热分解过程经历了3个阶段,其中间体和残余物运用TG-DTG、IR和XRD 技术进行了确证。采用Achar方程、Coats-Redfern方程、Kissinger方程、Flynn-Wall-Ozawa方程和Starink方程对非等温动力学数据进行了分析,得到了第3步热分解反应的机理函数、动力学参数和热分解反应动力学方程,其热分解反应过程受F3（化学反应）机理控制, 表观活化能为351 kJ·mol-1,指前因子为2.57×10 30s-1。