Hydrolyzed polyacrylamide grafted carboxymethylxyloglucan based microbeads for pH responsive drug delivery.
Hydrolyzed polyacrylamide grafted carboxymethylxyloglucan based microbeads for pH responsive drug delivery.
复制标题
DOI：
10.1016/j.ijbiomac.2014.03.005
复制
发表时间：
2014-06
影响因子：
8.2
通讯作者：
C. M. Setty;Anand S. Deshmukh;A. Badiger
中科院分区：
文献类型：
--
作者：
C. M. Setty;Anand S. Deshmukh;A. Badiger
本研究探讨了水解聚丙烯酰胺接枝羧甲基木葡聚糖（HPam-g-CMXG）的药物应用，作为有前途的聚合物材料的pH响应性微球的发展。采用传统的自由基聚合方法合成了接枝共聚物，并对其进行了皂化改性和表征。急性经口毒性研究确保了开发的共聚物用于临床应用的生物安全性。开发了不同批次的pH响应性球形微珠，并评价了工艺参数对其总体性能的影响。在两种不同pH介质（pH 1.2和pH 7.4）中进行的体外药物释放研究（USP Type-II，桨法）结果显示，所有制剂均呈现三相药物释放模式。与模拟胃（酸性）pH相比，微珠的药物释放和溶胀在模拟肠（碱性）pH中显著更高，并且这种性质对于靶向药物递送是期望的。在工艺参数和基质组成之间观察到强相关性，并且其直接影响药物转运机制。总之，水解聚丙烯酰胺接枝羧甲基木葡聚糖具有巨大的潜力，可作为新型基质材料用于靶向给药系统的设计。
The present study investigates the pharmaceutical application of hydrolyzed polyacrylamide grafted carboxymethylxyloglucan (HPam-g-CMXG), as promising polymeric material for the development of pH responsive microbeads. The graft copolymer was synthesized by conventional free radical polymerization method and saponified to enhance its functionality and characterized. An acute oral toxicity study ensured the bio-safety of developed copolymer for clinical application. Various batches of pH responsive spherical microbeads were developed and evaluated for the effect of process parameters on their overall performance. Result of in vitro drug release study (USP Type-II, paddle method) carried out in two different pH media (pH 1.2 and pH 7.4) showed a triphasic drug release pattern in all the formulations. Both the drug release and swelling of microbeads were significantly higher in simulated intestinal (alkaline) pH compared to simulated gastric (acidic) pH and this nature is desirable for targeted drug delivery. A strong correlation was observed between the process parameters and matrix composition and it directly influenced the drug transport mechanism. In conclusion, the hydrolyzed polyacrylamide grafted carboxymethylxyloglucan holds an immense potential to be explored pharmaceutically as new matrix material for the design of targeted drug delivery system.