Tavakol Moslem, Vasheghani-Farahani Ebrahim, Hashemi-Najafabadi Sameereh
Biotechnology Group, Faculty of Chemical Engineering, Tarbiat Modares University, P.O. Box 14115-143, Tehran, Iran.
Prog Biomater. 2013 Apr 4;2(1):10. doi: 10.1186/2194-0517-2-10.
In this study, pH-sensitive blended polymeric beads were prepared by ionic gelation of mixed alginate and N,O-carboxymethyl chitosan (NOCC) solutions in aqueous media containing calcium chloride. To prepare drug-loaded beads, sulfasalazine (SA) as a model drug was added to the initial aqueous polymer solution. These beads were characterized and evaluated in vitro as potential carriers for colon-specific drug delivery. A 3 full factorial experimental design was employed to evaluate the effect of polymer and CaCl concentrations on swelling and drug release behavior of the beads in simulated gastrointestinal tract fluid. It was found that the rate of swelling and drug release decreased significantly with increasing polymer and CaCl concentrations, but polymer concentration was more effective than CaCl concentration. The beads prepared using 4.5% polymer concentration and 4% CaCl concentration retained approximately 60% of the loaded drug before approaching the simulated colonic fluid. Based on the results, the alginate-NOCC beads prepared with high polymer concentration could be potentially suitable polymeric carriers for colon-specific delivery of SA.
在本研究中，通过在含有氯化钙的水性介质中对混合的海藻酸钠和N,O-羧甲基壳聚糖（NOCC）溶液进行离子凝胶化反应，制备了pH敏感的共混聚合物珠。为了制备载药珠，将作为模型药物的柳氮磺胺吡啶（SA）添加到初始的聚合物水溶液中。对这些珠子进行了表征，并在体外评估其作为结肠特异性药物递送潜在载体的性能。采用三因素全因子实验设计来评估聚合物和氯化钙浓度对珠子在模拟胃肠道液中的溶胀和药物释放行为的影响。结果发现，随着聚合物和氯化钙浓度的增加，溶胀率和药物释放率显著降低，但聚合物浓度比氯化钙浓度的影响更显著。使用4.5%聚合物浓度和4%氯化钙浓度制备的珠子在接近模拟结肠液之前保留了约60%的载药量。基于这些结果，用高聚合物浓度制备的海藻酸钠-NOCC珠可能是SA结肠特异性递送的潜在合适聚合物载体。
