Tulain Ume Ruqia, Ahmad Mahmood, Rashid Ayesha, Iqbal Furqan Muhammad
Acta Pol Pharm. 2016 Jul;73(4):1009-1022.
Present work concerned with development and evaluation of an innovative drug carrier, as smart drug delivery system for highly acid labile drug. Free radical polymerization technique was employed to develop pH sensitive drug delivery system by using carboxymethyl cellulose (polymer), methacrylic acid (monomer), potassium persulfate (initiator) and N,N methylene bisacrylamide (crosslinker). Prepared crosslinked polymer was characterized by swelling analysis at acidic and basic pH to evaluate pH responsive swelling, instrumental analysis (SEM, FIIR and thermal analysis) and pH responsive release of model drug rabeprazole sodium. Characterization of smart drug delivery concluded that pH responsive swelling and drug release parameters were directly related with methacrylic acid concentration in the crosslinked polymer. It was observed that by raising methacrylic acid contents swelling at basic pH enhanced and crosslinker contents increment reduce swelling. Among nine formulations with varying formulation contents, CMA2 exhibited more pH sensitive swelling and cumulative drug release at alkaline pH. Results of investigation recommended that CMA2 can be a best crosslinked polymer as smart drug carrier.
目前的工作涉及一种创新药物载体的开发和评估，该载体作为高度酸不稳定药物的智能给药系统。采用自由基聚合技术，使用羧甲基纤维素（聚合物）、甲基丙烯酸（单体）、过硫酸钾（引发剂）和N,N-亚甲基双丙烯酰胺（交联剂）来开发pH敏感给药系统。通过在酸性和碱性pH下的溶胀分析来表征制备的交联聚合物，以评估pH响应性溶胀、仪器分析（扫描电子显微镜、傅里叶变换红外光谱和热分析）以及模型药物雷贝拉唑钠的pH响应性释放。智能给药系统的表征得出结论，pH响应性溶胀和药物释放参数与交联聚合物中甲基丙烯酸的浓度直接相关。观察到，通过提高甲基丙烯酸含量，碱性pH下的溶胀增强，而交联剂含量的增加会降低溶胀。在九种具有不同配方含量的制剂中，CMA2在碱性pH下表现出更高的pH敏感性溶胀和累积药物释放。研究结果表明，CMA2可以作为一种最佳的交联聚合物作为智能药物载体。
