已经开发了一种有前途的受控药物递送系统,该系统基于使用不含药物的背衬层和含有硝苯地平的聚合物亲水性凝胶粘性芯层的聚合物粘性双层制剂。DSC热重分析证实了药物在凝胶层中的截留,并且没有显示潜在相互作用的证据。各种比例的生物粘附聚合物,包括HPMCK100,PVPK30,SCMC,和CP934与EC组合作为不可渗透的背衬层,以确保药物向颊粘膜的单向释放。亲水性凝胶状HPMC的聚合物组合物,SCMC,和CP在压缩过程中通过包围核心硝苯地平形成基质层。对所有成分进行预配制研究以评价其物理和流动特性。离体生物粘合强度,表面pH值,肿胀指数,体外和体内药物释放,进行和离体渗透研究以评价产生的基于凝胶的系统。快速的温度变化对物质的物理性质没有明显的影响,药理含量,或在使用实际人类唾液进行稳定性测试期间的亲粘强度。从离体粘膜的组织学检查可以清楚地看出,开发的系统在给药部位没有引起任何刺激或炎症。配方NT5是最好的,相关系数为0.9966。体外和体内药物释放曲线具有良好的相关性,它们通过生物膜模拟体外药物释放模式。因此,开发的基于凝胶的配方被发现是新颖的,稳定,并可用于硝苯地平的靶向递送。
A promising controlled drug delivery system has been developed based on polymeric buccoadhesive bilayered formulation that uses a drug-free backing layer and a polymeric hydrophilic gel buccoadhesive core layer containing nifedipine. The DSC thermogravimetric analysis confirms the drug\'s entrapment in the gel layer and reveals no evidence of a potential interaction. Various ratios of bioadhesive polymers, including HPMC K100, PVP K30, SCMC, and CP 934, were combined with EC as an impermeable backing layer to ensure unidirectional drug release towards the buccal mucosa. The polymeric compositions of hydrophilic gel-natured HPMC, SCMC, and CP formed a matrix layer by surrounding the core nifedipine during compression. Preformulation studies were performed for all of the ingredients in order to evaluate their physical and flow characteristics. Ex vivo buccoadhesive strength, surface pH, swelling index, in vitro and in vivo drug release, and ex vivo permeation investigations were performed to evaluate the produced gel-based system. Rapid temperature variations had no appreciable impact on the substance\'s physical properties, pharmacological content, or buccoadhesive strength during stability testing using actual human saliva. It was clear from a histological examination of the ex vivo mucosa that the developed system did not cause any irritation or inflammation at the site of administration. The formulation NT5 was the best one, with a correlation coefficient of 0.9966. The in vitro and in vivo drug release profiles were well correlated, and they mimic the in vitro drug release pattern via the biological membrane. Thus, the developed gel-based formulation was found to be novel, stable, and useful for the targeted delivery of nifedipine.