Sun Xiaodong, Qiu Haiying, Jin Yiguang
Pharmaceutical College of Henan University, Kaifeng 475004, China; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 27 Taiping Road, Beijing 100850, China.
Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 27 Taiping Road, Beijing 100850, China.
Int J Pharm. 2017 Jun 15;525(1):175-182. doi: 10.1016/j.ijpharm.2017.04.026. Epub 2017 Apr 13.
Aerobic vaginitis (AV) leads to uterus deep infection or preterm birth. Antibacterial agents are not optimal therapeutics of AV. Here, we report a series of temperature-sensitive in situ forming acidic buffered gels for topical treatment of AV, involving lactate, acetate, and citrate gels at pH 3.5, 5.0, and 6.5. AV rat models were prepared following vaginal infection with Staphylococcus aureus and Escherichia coli. In vitro/in vivo studies of the buffered gels were performed compared with ofloxacin gels and blank gels. All the buffered gels showed the lower in vitro antibacterial activities than ofloxacin gels but the better in vivo anti-S. aureus effects and similar anti-E. coli effects. The buffered gels improved Lactobacillus growth in the vaginas. Both the healthy rat vaginal pH and the pH of rat vaginas treated with the buffered gels were about 6.5 though the AV rat models or ones treated with ofloxacin gels still remained at the high pH more than 7.0. After treatments with the buffered gels, the vaginal smears changed to a clean state nearly without aerobic bacteria, the vaginal tissues were refreshed, and the immunoreactions were downregulated. The acidic buffered gels bring rapid decrease of local vaginal pH, high antibacterial activities, improvement of probiotics, and alleviation of inflammation. They are simple, highly efficient, and safe anti-AV formulations.
需氧性阴道炎(AV)可导致子宫深部感染或早产。抗菌药物并非治疗AV的最佳疗法。在此,我们报告了一系列用于局部治疗AV的温度敏感型原位形成酸性缓冲凝胶,包括pH值为3.5、5.0和6.5的乳酸盐、醋酸盐和柠檬酸盐凝胶。通过阴道感染金黄色葡萄球菌和大肠杆菌制备AV大鼠模型。将缓冲凝胶与氧氟沙星凝胶和空白凝胶进行体外/体内研究比较。所有缓冲凝胶的体外抗菌活性均低于氧氟沙星凝胶,但体内抗金黄色葡萄球菌效果更好,抗大肠杆菌效果相似。缓冲凝胶促进了阴道内乳酸杆菌的生长。尽管AV大鼠模型或用氧氟沙星凝胶治疗的大鼠阴道pH值仍高于7.0,但健康大鼠阴道pH值和用缓冲凝胶治疗的大鼠阴道pH值均约为6.5。用缓冲凝胶治疗后,阴道涂片几乎没有需氧菌,变为清洁状态,阴道组织恢复活力,免疫反应下调。酸性缓冲凝胶可使局部阴道pH值迅速降低,具有高抗菌活性,改善益生菌状况并减轻炎症。它们是简单、高效且安全的抗AV制剂。