Department of Life Sciences, National Taiwan Ocean University, Keelung, Taiwan, ROC.
J Mater Sci Mater Med. 2013 Feb;24(2):317-23. doi: 10.1007/s10856-012-4798-9. Epub 2012 Oct 27.
The purposes of this study were to develop and evaluate calcium pectinate/alginate microspheres (PAMs) and to exploit their pH-sensitive properties for colon-targeted delivery of encapsulated cisplatin. PAMs were prepared using an electrospraying method. The PAMs, as cores, were then coated with Eudragit S100 using a polyelectrolyte multilayer coating technique in aqueous solution. The morphology of the microspheres was observed under scanning electron microscopy. In vitro drug release studies were performed in simulated gastrointestinal fluid, and the results indicated that approximately 5 % of the cisplatin was released from the Eudragit S100-coated PAMs, and 51 % of the cisplatin was released from the uncoated PAMs at 1 h. The release of cisplatin from the Eudragit S100-coated PAMs was more sustained in simulated gastric fluid than in simulated intestinal fluid due to the increased solubility of the coating polymer in media with pH >7.0. Drug release from the Eudragit S100-coated PAMs was best described by the Higuchi's square root model. From these results, it was concluded that Eudragit S100-coated PAMs are a potential carrier for delivery of cisplatin to the colon.
本研究旨在开发和评价海藻酸钙/海藻酸钠微球（PAMs），并利用其 pH 敏感性将包裹的顺铂递送至结肠。PAMs 是采用电喷雾方法制备的。然后，将 PAMs 作为核，采用聚电解质多层涂层技术在水溶液中用 Eudragit S100 进行包衣。通过扫描电子显微镜观察微球的形态。在模拟胃肠道液中进行体外药物释放研究，结果表明，在 1 小时时，约有 5%的顺铂从 Eudragit S100 包衣的 PAMs 中释放，而 51%的顺铂从未包衣的 PAMs 中释放。由于涂层聚合物在 pH 值大于 7.0 的介质中的溶解度增加，因此 Eudragit S100 包衣的 PAMs 中顺铂的释放更持续在模拟胃液中而不是在模拟肠液中。Eudragit S100 包衣的 PAMs 中的药物释放最符合 Higuchi 的平方根模型。从这些结果可以得出结论，Eudragit S100 包衣的 PAMs 是将顺铂递送至结肠的潜在载体。
