Khan Samiullah, Rehman Abdur, Badshah Syed Faisal, Shazly Gamal A, Metouekel Amira, Dabiellil Fakhreldeen
College of Pharmacy, Margalla Institute of Health Sciences, Islamabad, Pakistan.
College of Pharmaceutical Sciences, Soochow University, Suzhou, China.
Des Monomers Polym. 2024 Dec 30;28(1):1-15. doi: 10.1080/15685551.2024.2442118. eCollection 2025.
Ibuprofen sodium (IBP) is a commonly used NSAID for multiple pain conditions. However, despite its extensive use, it is associated with multiple GIT adverse effects after oral administration. In the present study, we have fabricated thermoresponsive gel depot using Poly (N-vinylcaprolactam) and sodium alginate as polymers. The designed formulations are intended to be used as IBP depot after being administered subcutaneously. The sol-gel phase transition temperature and gelation time of gel samples were optimized by tube inversion, rheological exploration and optical transmittances. Temperature sweep experiments confirmed that optimized gel samples have sol-gel transition between 32°C and 37°C. Swelling and drug release displayed that optimized gels have maximum swelling and IBP release at pH 7.4 and at 35°C confirming their pH/thermo sensitivity. The degradation profile of hydrogels displayed controlled degradation for 6 days that with increasing contents. MTT assay showed L929 cells displayed more than 90% cell viability against blank and IBP-loaded PNVCL/NaAlg hydrogels at optimized concentrations. Fourier transform infrared spectroscopy confirmed the polymer blend hydrogels structure formation. Thermogravimetric analysis confirmed the presence of thermoresponsive moieties and thermal stability of polymer blend hydrogel sample. While scanning electron microscopy showed that hydrogel has channels in structure that might facilitate the diffusion of solvent. Results concluded that PNVCL/NaAlg hydrogels can be utilized as IBP sustained depot following subcutaneous application and GIT adverse effects could be avoided associated with its oral administration.
布洛芬钠（IBP）是一种常用于多种疼痛病症的非甾体抗炎药。然而，尽管其广泛使用，但口服后会引发多种胃肠道不良反应。在本研究中，我们使用聚（N - 乙烯基己内酰胺）和海藻酸钠作为聚合物制备了热响应性凝胶制剂。设计的制剂旨在皮下给药后用作IBP制剂。通过试管倒置、流变学探索和透光率对凝胶样品的溶胶 - 凝胶相变温度和凝胶化时间进行了优化。温度扫描实验证实，优化后的凝胶样品在32°C至37°C之间发生溶胶 - 凝胶转变。溶胀和药物释放表明，优化后的凝胶在pH 7.4和35°C时具有最大溶胀和IBP释放，证实了它们的pH/热敏感性。水凝胶的降解曲线显示，随着含量增加，其降解可控达6天。MTT试验表明，在优化浓度下，L929细胞对空白和负载IBP的PNVCL/NaAlg水凝胶的细胞活力超过90%。傅里叶变换红外光谱证实了聚合物共混水凝胶结构的形成。热重分析证实了聚合物共混水凝胶样品中热响应部分的存在及其热稳定性。而扫描电子显微镜显示水凝胶结构中有通道，这可能有助于溶剂的扩散。结果表明，PNVCL/NaAlg水凝胶皮下给药后可作为IBP缓释制剂，避免口服给药相关的胃肠道不良反应。
