Vignan Pharmacy College, Vadlamudi, Guntur, AP 522213, India.
Vignan Pharmacy College, Vadlamudi, Guntur, AP 522213, India.
Int J Biol Macromol. 2019 Oct 15;139:320-331. doi: 10.1016/j.ijbiomac.2019.07.190. Epub 2019 Jul 30.
The present work investigates a blend of Linum Seed mucilage(LSM) and Hibiscus Leaf gum(HLG) as mucoadhesive carriers for Capecitabine(CPTB) loaded mucoadhesive composite bead formulation (CMB), in an attempt to achieve sustained release of CPTB (BCS Class I drug) in the colon region. Optimization using Box-Behnken Design(BBD) was used to study the effect of quantities of mucoadhesive carriers(LSM,HLG) and enteric polymer pectin (in curing solution) on response factors such as %drug loading (%DL) and %drug release (%DR). CMB prepared by ion-gelation technique showed uniform bead size, spherical surface morphology, maximum drug encapsulation efficiency. The optimized CMB(F18) exhibited maximum %drug loading(28.94%), favorable in vitro drug release of CPTB(54.43%) in 12 h, where, the release kinetics follow zero order non-Fickian diffusion mechanism. CMB's exhibited significantly higher swelling upon exposure to alkaline media than acidic media similarly ex vivo mucoadhesive study also revealed that major fraction of beads were washed off within 2 h in 1.2pH media whereas in 7.4pH alkaline media major portion of the beads remain adhered even after 24 h Moreover accelerated stability testing of CMB(F18) revealed shelf life of about 2.59 years. Hence the study confirms that the combination of LSM&HLG as ideal mucoadhesive carriers and can favorably target highly soluble drugs to the colon region.
本研究考察了亚麻籽胶（LSM）和芙蓉叶胶（HLG）的混合物作为卡培他滨（CPTB）载药的粘膜粘附复合珠粒制剂（CMB）的粘膜粘附载体，旨在实现CPTB（BCS 类 I 药物）在结肠区域的持续释放。Box-Behnken 设计（BBD）用于研究粘膜粘附载体（LSM、HLG）和肠溶性聚合物果胶（在固化溶液中）的用量对响应因子（如载药量（%DL）和药物释放（%DR）的影响。离子凝胶技术制备的 CMB 具有均匀的珠粒粒径、球形表面形态和最大的药物包封效率。优化后的 CMB（F18）显示出最大的载药量（28.94%），有利于 CPTB 在 12 小时内释放（54.43%），其中释放动力学遵循零级非菲克扩散机制。CMB 在暴露于碱性介质时表现出明显更高的溶胀性，而在酸性介质中则没有。同样，体外粘膜粘附研究也表明，在 1.2pH 介质中，大部分珠粒在 2 小时内被冲洗掉，而在 7.4pH 碱性介质中，即使在 24 小时后，大部分珠粒仍保持粘附。此外，CMB（F18）的加速稳定性测试表明其保质期约为 2.59 年。因此，该研究证实，LSM 和 HLG 的组合是理想的粘膜粘附载体，可以将高水溶性药物靶向结肠区域。
