Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t_50%, t_90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

目前的研究旨在合成和表征壳聚糖-邻苯二酚共轭物，并设计和开发载有拉富替丁的粘膜粘附药丸。SEM图像表明存在纤维结构，该结构负责壳聚糖-邻苯二酚缀合物的粘膜粘附潜能的增强。分别通过DSC和XRD研究证实了缀合物的热力学稳定性和无定形性质。流变学研究用于评估聚合物粘蛋白的相互作用，其中与原始的壳聚糖和粘蛋白相比，壳聚糖-邻苯二酚共轭物和粘蛋白之间观察到强相互作用。使用分子力学模拟在计算机上评估了壳聚糖-邻苯二酚（Cht-C）与壳聚糖（Cht）的粘膜粘附潜能，并将所得结果与体外和离体结果进行了比较。Cht-C /粘蛋白显示出比Cht /粘蛋白分子复合物更高的能量稳定度（∆E≈-65 kcal / mol）。由壳聚糖（LPC）和壳聚糖-邻苯二酚缀合物（LPCC）制备负载拉夫替丁的丸剂，并评价各种物理性质，即。流动性，圆度，圆度，易碎性，药物含量，粒度和粘膜粘附百分比。对LPC和LPCC药丸进行了体外药物释放研究，用于计算t _50％，t _90％和平均溶解时间。据报道，对于LPC和LPCC药丸，Korsmeyer-Peppas模型的释放指数值分别为0.443和0.759，表明分别代表药物释放的Fickian和非Fickian机理。体内结果显示从壳聚糖-邻苯二酚包衣的小丸中释放后，药物具有明显的控制释放和增强的滞留性。发现壳聚糖-邻苯二酚缀合物是用于开发各种粘膜粘附制剂的有前途的生物粘附聚合物。