Sinha Priyanka, Ubaidulla U, Hasnain M Saquib, Nayak Amit Kumar, Rama Bobba
Department of Pharmaceutics, C. L. Baid Metha College of Pharmacy, Jyothi Nagar, Rajiv Gandhi Salai, Thorapakkam, Chennai 600097, India.
Department of Pharmacy, B. B. S. Institute of Pharmaceutical and Allied Science, Greater Noida 201310, India.
Int J Biol Macromol. 2015 Aug;79:555-63. doi: 10.1016/j.ijbiomac.2015.04.067. Epub 2015 May 15.
Zinc (Zn(2+))-ion induced diclofenac sodium (DS)-loaded alginate-okra (Hibiscus esculentus) gum (OG) blend beads was successfully formulated through Zn(2+)-ion induced ionic-gelation cross-linking method in a complete aqueous environment. Effects of polymer-blend ratio and cross-linker concentration on drug encapsulation efficiency (DEE) and cumulative drug release at 8 h (R8h) were optimized by 3(2)-factorial design. The optimized formulation of Zn(2+)-ion induced DS-loaded alginate-OG beads demonstrated 89.27±3.58% of DEE and 43.73±2.83% of R8h. The bead sizes were within 1.10±0.07 to 1.38±0.14 mm. The bead surface morphology was analyzed by SEM. The drug-polymer interaction in the optimized bead matrix was analyzed by FTIR and P-XRD. These beads exhibited sustained in vitro drug release over a prolonged period of 8h and followed controlled-release (zero-order) pattern with super case-II transport mechanism. The swelling and degradation of the optimized beads was influenced by the pH of test mediums, which might be suitable for intestinal drug delivery.
通过锌（Zn(2+)）离子诱导的离子凝胶交联法，在完全水性环境中成功制备了负载双氯芬酸钠（DS）的海藻酸钠-秋葵（Hibiscus esculentus）胶（OG）共混珠。采用3(2)析因设计优化了聚合物共混比例和交联剂浓度对药物包封率（DEE）和8小时累积药物释放率（R8h）的影响。锌离子诱导的负载DS的海藻酸钠-OG珠的优化制剂显示出89.27±3.58%的DEE和43.73±2.83%的R8h。珠粒尺寸在1.10±0.07至1.38±0.14毫米之间。通过扫描电子显微镜（SEM）分析珠粒表面形态。通过傅里叶变换红外光谱（FTIR）和粉末X射线衍射（P-XRD）分析优化后的珠粒基质中的药物-聚合物相互作用。这些珠粒在长达8小时的时间内表现出持续的体外药物释放，并遵循具有超Ⅱ型转运机制的控释（零级）模式。优化后的珠粒的溶胀和降解受测试介质pH值的影响，这可能适用于肠道给药。
