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Encapsulation of ciprofloxacin within modified xanthan gum- chitosan based hydrogel for drug delivery.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-11-22 , DOI: 10.1016/j.bioorg.2018.11.036
Demiana H Hanna 1 , Gamal R Saad 1
Affiliation  

The aim of the present work was to investigate the preparation of polyelectrolyte hydrogel as potential drug carrier for antibacterial Ciprofloxacin drug (CFX), intended for controlled release formulation. Hydrogel of N-trimehtyl chitosan (TMC)/sodium carboxymethyl xanthan gum (CMXG) was prepared and ciprofloxacin was employed as a model drug to investigate the loading and release performance of the prepared hydrogel. FTIR, DSC, TGA and SEM analysis were used to characterize the TMC/CMXG hydrogel and its CFX loaded hydrogel. The results showed that the ciprofloxacin was successfully incorporated and released from the prepared hydrogel without the loss of structural integrity or the change in its functionality. The encapsulation efficiency of CFX within the prepared hydrogel was found to be increased with increasing the concentration of drug reaching about 93.8 ± 2.1% with concentration of CFX 250 µg/ml. It was shown also that the drug is entrapped within the gel without significant interaction as confirmed from FTIR spectra and DSC analysis. In vitro release study in phosphate buffer saline (PBS), indicated the steady rise in cumulative drug release with the highest release amount, reaching about 96.1 ± 1.8% up to 150 min, whereby the gel with high drug loading efficiency (3.52 ± 0.07%) displayed faster and higher release rate than that of gel containing a smaller amount of drug (0.44 ± 0.01%). The release kinetics of loaded drug followed zero-order kinetics. CFX drug loaded hydrogel showed high activity against the gram positive and gram negative bacterial strains due to the successful released of CFX from the CFX loaded hydrogel into the tested bacterial strains with the highest diameter of inhibition zone against Escherichia coli (67.0 ± 1.0) as compared to reference antibiotic, Gentamicin (28 ± 0.5). Cytotoxicity of the prepared hydrogel was examined in vitro using lung human normal cell lines and showed the highest cell viability (97 ± 0.5%) at concentration up to 50 µg/ml. Consequently, TMC/CMXG hydrogel can be proposed as new controlled release drug delivery system.

中文翻译:

环丙沙星在修饰的以黄原胶-壳聚糖为基的水凝胶中的封装,用于药物递送。

本工作的目的是研究聚电解质水凝胶的制备,将其作为抗菌药物环丙沙星药物(CFX)的潜在药物载体,用于控释制剂。制备了N-三甲基壳聚糖(TMC)/羧甲基黄原胶钠(CMXG)的水凝胶,并以环丙沙星为模型药物研究了制备的水凝胶的负载和释放性能。FTIR,DSC,TGA和SEM分析用于表征TMC / CMXG水凝胶及其载有CFX的水凝胶。结果表明,环丙沙星可以成功地掺入并从制备的水凝胶中释放出来,而不会丧失结构完整性或功能性的改变。发现当CFX浓度为250 µg / ml时,随着药物浓度的增加,CFX的封装效率会提高,达到约93.8±2.1%。还显示如FTIR光谱和DSC分析所证实的,药物被包埋在凝胶中而没有明显的相互作用。在磷酸盐缓冲盐水(PBS)中进行的体外释放研究表明,累积的药物释放以最高的释放量稳步上升,在150分钟内达到约96.1±1.8%,从而凝胶具有高载药率(3.52±0.07%) )的释放速率比含少量药物(0.44±0.01%)的凝胶释放速率更高。加载药物的释放动力学遵循零级动力学。载有CFX药物的水凝胶对革兰氏阳性和革兰氏阴性细菌菌株显示出高活性,这是因为与载有CFX的水凝胶相比,CFX成功地从载有CFX的水凝胶中释放到测试菌株中,具有最大的对大肠杆菌的抑制区直径(67.0±1.0)参考庆大霉素(28±0.5)。使用肺人类正常细胞系在体外检查了制备的水凝胶的细胞毒性,在浓度高达50 µg / ml时显示出最高的细胞活力(97±0.5%)。因此,TMC / CMXG水凝胶可被提议作为新的控释药物递送系统。庆大霉素(28±0.5)。使用肺人类正常细胞系在体外检查了制备的水凝胶的细胞毒性,在浓度高达50 µg / ml时显示出最高的细胞活力(97±0.5%)。因此,TMC / CMXG水凝胶可被提议作为新的控释药物递送系统。庆大霉素(28±0.5)。使用肺人类正常细胞系在体外检查了制备的水凝胶的细胞毒性,在浓度高达50 µg / ml时显示出最高的细胞活力(97±0.5%)。因此,TMC / CMXG水凝胶可被提议作为新的控释药物递送系统。
更新日期:2018-11-22
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