Abstract：
A skin wound is prone to bacterial infection and growth. An antibacterial topical hydrogel that can act as a self-drug-delivery (SDD) system is reported here. Two bidentate ligands (L2/L1) derived from imidazole/benzimidazole derivatives when reacted with Zn(NO3)2 and a series of nonsteroidal-anti-inflammatory drugs (NSAIDs) produced crystalline products, which were characterized by single-crystal X-ray diffraction (SXRD). Simple mixing of the ingredients of the crystalline products (stoichiometry guided by the corresponding crystal structure) produced an aqueous gel (DMSO/water) when the bidentate ligand was water-insoluble L2, whereas water-soluble L1 readily produced hydrogels under similar conditions. Dynamic rheology and scanning electron microscopy (SEM) were employed to characterize the gels. Zone inhibition diameters, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and hemolysis data suggested that among the hydrogelators, L1MEC derived from L1, meclofenac and Zn(NO3)2, was found to be the best against the Gram-negative bacteria Escherichia coli. The corresponding hydrogel L1MEC_HG and a piece of a dried cloth bandage coated with the hydrogel also showed appreciable activity against E. coli. The antibacterial property of L1MEC_HG against E. coli, thus demonstrated, is relevant in developing an antibacterial SDD system because E. coli is reported to be present in infected wounds.
摘要：
皮肤伤口易于细菌感染和生长。这里报道了一种抗菌局部水凝胶,其可以充当自药物递送(SDD)系统。当与Zn（NO3）2和一系列非甾体抗炎药（NSAID）反应时，由咪唑/苯并咪唑衍生物衍生的两个双齿配体（L2/L1）产生结晶产物，用单晶X射线衍射(SXRD)对其进行了表征。当二齿配体是水不溶性L2时，结晶产物的成分的简单混合（化学计量由相应的晶体结构指导）产生了水性凝胶（DMSO/水），而水溶性L1在类似条件下容易产生水凝胶。采用动态流变学和扫描电子显微镜（SEM）表征凝胶。区域抑制直径,最小抑制浓度（MIC），最小杀菌浓度（MBC），溶血数据表明，在水凝胶剂中，发现来自L1，甲氯芬酸和Zn（NO3）2的L1MEC对革兰氏阴性菌大肠杆菌最好。相应的水凝胶L1MEC_HG和涂覆有水凝胶的干布绷带片也显示出明显的抗大肠杆菌活性。L1MEC_HG对大肠杆菌的抗菌性能,由此证明，与开发抗菌SDD系统有关，因为据报道大肠杆菌存在于感染的伤口中。
