Alagusundaram M, Jain Nem Kumar, Begum M Yasmin, Parameswari S Angala, Nelson Vinod Kumar, Bayan Mohammad F, Chandrasekaran Balakumar
Department of Pharmaceutics, School of Pharmacy, ITM University, Gwalior 474001, Madhya Pradesh, India.
Department of Pharmacology, School of Pharmacy, ITM University, Gwalior 474001, Madhya Pradesh, India.
Gels. 2023 Aug 26;9(9):688. doi: 10.3390/gels9090688.
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.
基于聚合物口腔黏附双层制剂开发了一种有前景的控释给药系统,该制剂使用无药背衬层和含有硝苯地平的聚合物亲水性凝胶口腔黏附核心层。差示扫描量热法热重分析证实药物包封在凝胶层中,且未发现潜在相互作用的证据。将包括羟丙甲纤维素K100、聚乙烯吡咯烷酮K30、羧甲基纤维素钠和卡波姆934在内的各种生物黏附聚合物比例与乙基纤维素作为不透性背衬层相结合,以确保药物单向释放至颊黏膜。亲水性凝胶性质的羟丙甲纤维素、羧甲基纤维素钠和卡波姆的聚合物组合物在压制过程中通过包围核心硝苯地平形成基质层。对所有成分进行了处方前研究,以评估其物理和流动特性。进行了体外口腔黏附强度、表面pH值、溶胀指数、体外和体内药物释放以及体外渗透研究,以评估所制备的基于凝胶的系统。在使用实际人唾液进行稳定性测试期间,快速温度变化对该物质的物理性质、药理含量或口腔黏附强度没有明显影响。从体外黏膜的组织学检查可以清楚地看出,所开发的系统在给药部位未引起任何刺激或炎症。制剂NT5是最佳制剂,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,并且它们模拟了通过生物膜的体外药物释放模式。因此,所开发的基于凝胶的制剂被发现是新颖、稳定且可用于硝苯地平的靶向递送。