...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Open Pharmaceutical Sciences Journal >Water Soluble Chitosan Mediated Voriconazole Microemulsion as Sustained Carrier for Ophthalmic Application: In vitro/Ex vivo/In vivo Evaluations
【24h】

Water Soluble Chitosan Mediated Voriconazole Microemulsion as Sustained Carrier for Ophthalmic Application: In vitro/Ex vivo/In vivo Evaluations

机译：水溶性壳聚糖介导的伏立康唑微乳剂作为眼科应用的持续载体：体外/离体/体内评价

获取原文
   

获取外文期刊封面封底 >>

       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Background:Voriconazole (VCZ) is a lipophilic candidate, effective against fungal infections like ocular keratitis and endopthalmitis.Objective:The purpose to develop, optimize and characterize voriconazole microemulsion as sustained medication for ophthalmic application.Methods:The pseudo-ternary phase diagrams were developed using oleic acid, isopropyl myristate and isopropyl palmitate (oil phases), tween 80 (surfactant), propylene glycol (co-surfactant), distilled water (aqueous phase) and modified chitosan (Mod.CH) as mucoadhesive polymer. The optimum composition of oil, S_(mix) and water was selected on the basis of phase diagrams and as mucoadhesive polymer Mod.CH was used in the formulations. All the formulations were evaluated for thermodynamic stability/dispersibility, physicochemical parameters (droplet size, polydispersity index, zeta potential, drug content, viscosity, pH and conductivity), in vitro , ex vivo and in vivo studies.Results:All formulations showed droplet size below 250 nm, positive zeta potential and polydispersity index below 0.5. The in vitro drug release study performed on selected formulations showed maximum sustained release than marketed formulation. The in vitro transcorneal permeation experiment of formulations suggests that optimized formulations showed better permeation. The selected formulation of voriconazole microemulsion was able to produce maximum antifungal activity against Candida albicans when compared to marketed formulation. In vivo study performed on rabbit eyes, found more drug concentration in aqueous humor of optimized formulation; the AUC_(0→)_(t) of IPMVM-11 was approximately 6.84-fold higher than VOZOLE and efficiently enhanced the corneal bioavailability.Conclusion:The modified chitosan based on voriconazole loaded microemulsion was promising novel carrier for sustained action in ophthalmic medication.
机译：背景：伏立康唑（VCZ）是一种亲脂性候选物，对眼部角膜炎和眼内炎等真菌感染有效。目的：开发，优化和表征伏立康唑微乳剂作为眼科用药的持久药物方法：开发伪三元相图使用油酸，肉豆蔻酸异丙酯和棕榈酸异丙酯（油相），吐温80（表面活性剂），丙二醇（助表面活性剂），蒸馏水（水相）和改性壳聚糖（Mod.CH）作为粘膜粘附聚合物。根据相图选择油，S_（混合）和水的最佳组成，并且在配方中使用了粘膜粘附聚合物Mod.CH。评价所有制剂的热力学稳定性/分散性，理化参数（液滴大小，多分散性指数，ζ电位，药物含量，粘度，pH和电导率），体外，体外和体内结果：所有制剂的液滴尺寸均低于250 nm，ζ电位为正，多分散指数低于0.5。在选定的制剂上进行的体外药物释放研究显示出比市售制剂最大的持续释放。制剂的体外经角膜渗透实验表明，优化的制剂表现出更好的渗透性。与市售制剂相比，伏立康唑微乳液的选定制剂能够对白念珠菌产生最大的抗真菌活性。在兔眼上进行的体内研究发现，优化配方的房水中药物浓度更高; IPMVM-11的AUC_（0→）i_（t）约为VOZOLE的6.84倍，并有效地增强了角膜的生物利用度。结论：基于伏立康唑的微乳液修饰的壳聚糖有望成为新型的持续作用载体。眼科用药。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号