Abstract：
The crosslinking of the polymer matrix with compatible macromolecules results in a three-dimensional network structure that offers an enhancement in the controlled release properties of the material. In this sense, this work aimed to improve the release profile of mefenamic acid (MAC) through crosslinking strategies. κ-Carrageenan/sericin crosslinked blend was obtained by covalent and thermal crosslinking and the different formulations were characterized. The gastroresistant potential and release profile were evaluated in the dissolution assay. The effect and characterization of the particles were investigated. Multiple units presented high entrapment efficiency (94.11-104.25), high drug loading (36.50-47.50 %) and adequate particle size (1.34-1.57 mm) with rough surface and visually spherical shape. The Weibull model showed that drug release occurred by relaxation, erosion and Fickian diffusion. Material stability and absence of MAC -polymer interactions were demonstrated by FTIR and thermogravimetric analysis. DSC showed a stable character of MAC in the drug-loaded beads. Moreover, the application studies of κ-Car/Ser/carboxymethylcellulose in the in vitro intestine mode showed that the crosslinked blend increased cell viability (>85 %), while free MAC exhibited a cytotoxic effect. Finally, the crosslinked k-Car/Ser blend MAC -loaded showed promising properties of a sustained release form of anti-inflammatory drug.
摘要：
聚合物基质与相容大分子的交联导致三维网络结构,其提供材料的控制释放性质的增强。在这个意义上,这项工作旨在通过交联策略改善甲芬那酸（MAC）的释放曲线。通过共价和热交联获得κ-角叉菜胶/丝胶交联的共混物，并表征了不同的配方。在溶出度测定中评估了胃抗性潜力和释放曲线。研究了颗粒的作用和表征。多个单元呈现高截留效率(94.11-104.25)，高载药量（36.50-47.50%）和足够的粒径（1.34-1.57mm），表面粗糙，视觉上呈球形。Weibull模型表明，药物释放是通过松弛发生的，侵蚀和Fickian扩散。通过FTIR和热重分析证明了材料的稳定性和不存在MAC-聚合物相互作用。DSC在载药珠子中显示MAC的稳定特性。此外，κ-Car/Ser/羧甲基纤维素在体外肠道模式中的应用研究表明，交联混合物增加了细胞活力（>85％），而游离MAC表现出细胞毒性作用。最后,交联的k-Car/Ser共混物MAC负载显示出持续释放形式的抗炎药物的有希望的性质。
