Departamento de Farmacia y Tecnología Farmacéutica y Parasitología, Facultad de Farmacia. Universitat de València. Av. Vicente Andrés Estelles s/n, Burjassot, Valencia, Spain; Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València. Av. Vicente Andrés Estelles s/n, Burjassot, Valencia, Spain.
Departamento de Farmacia y Tecnología Farmacéutica y Parasitología, Facultad de Farmacia. Universitat de València. Av. Vicente Andrés Estelles s/n, Burjassot, Valencia, Spain.
Colloids Surf B Biointerfaces. 2019 Sep 1;181:1-5. doi: 10.1016/j.colsurfb.2019.05.024. Epub 2019 May 11.
Development of a pharmaceutical form for the superficial infections related with arthroplasties would be helpful for clinical practice. In this context, we set out to evaluate ciprofloxacin and gentamicin elution from systems based on chitosan. Films and semisolid hydrogels containing chitosan alone (2%) or in combination with gelatin (6%) or different proportions (from 12% to 36%) of tetrakis-(hydroxymethyl)-phosphonium-chloride (THPC) were tested as delivery systems. Different antibiotic doses were assayed (0.5 mg/cm,1 mg/cm and 2 mg/cm). Antibiotic release was studied for each formulation. In vitro cytocompatibility studies and a simulation exercise for bioactivity evaluation were performed. Samples containing chitosan or chitosan-gelatin released the antibiotics at very high rates. On the contrary, ciprofloxacin released was kept for 6 days from THPC-chitosan films and hydrogels. From hydrogel formulations release could be changed by varying the percentage of THPC. The system containing 12%-THPC-chitosan with 2 mg/cm of ciprofloxacin showed that 100% of patient would be covered during 72 h post-surgery. The concentration of 12%-THPC did not show cytotoxicity in NIH3T3 mouse fibroblasts after 48 h. THPC is suitable as crosslinker for chitosan when ciprofloxacin is incorporated showing a sustained release during 6 days.
开发一种用于治疗关节置换术后浅表感染的药物剂型将有助于临床实践。在这方面,我们着手评估基于壳聚糖的系统中环丙沙星和庆大霉素的洗脱情况。测试了含有壳聚糖(2%)或与明胶(6%)或不同比例(从 12%到 36%)四羟甲基氯化鏻(THPC)的壳聚糖单独或组合的薄膜和半固体水凝胶作为递送系统。测试了不同的抗生素剂量(0.5mg/cm、1mg/cm 和 2mg/cm)。研究了每种制剂的抗生素释放情况。进行了体外细胞相容性研究和生物活性评估模拟实验。含有壳聚糖或壳聚糖-明胶的样品以非常高的速度释放抗生素。相反,THPC-壳聚糖薄膜和水凝胶可在 6 天内保持释放环丙沙星。通过改变 THPC 的百分比,可以改变水凝胶制剂的释放。含有 12%-THPC-壳聚糖和 2mg/cm 环丙沙星的水凝胶制剂表明,在术后 72 小时内,100%的患者将得到覆盖。在 NIH3T3 小鼠成纤维细胞中,THPC 浓度在 48 小时后没有显示出细胞毒性。当将环丙沙星掺入壳聚糖中时,THPC 适合作为交联剂,可在 6 天内持续释放。