Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
J Microencapsul. 2011;28(7):659-67. doi: 10.3109/02652048.2011.604436. Epub 2011 Aug 9.
Currently, colon-specific drug delivery systems have been investigated for drugs that can exert their bioactivities in the colon. In this study, Eudragit® S100 coated calcium pectinate microsphere, a pH-dependent and enzyme-dependent system, as colon-specific delivery carrier for curcumin was investigated. Curcumin-loaded calcium pectinate microspheres were prepared by emulsification-linkage method, and the preparation technology was optimised by uniform experimental design. The morphology of microspheres was observed under scanning electron microscopy. Interactions between drug and polymers were investigated with differential scanning calorimetry (DSC) and X-ray diffraction. In vitro drug release studies were performed in simulated colonic fluid in the presence of Pectinex Ultra SP-L or 1% (w/v) rat caecal content, and the results indicated that the release of curcumin was significantly increased in the presence of 1% (w/v) rat caecal contents. It could be concluded that Eudragit® S100 coated calcium pectinate microsphere was a potential carrier for colon delivery of curcumin.
目前,人们已经研究了用于在结肠发挥生物活性的药物的结肠特异性药物传递系统。在这项研究中,考察了 Eudragit® S100 包衣的果胶酸钙微球作为姜黄素的 pH 依赖性和酶依赖性结肠特异性传递载体。通过乳化-连接法制备载姜黄素的果胶酸钙微球,并通过均匀实验设计优化了制备工艺。扫描电子显微镜观察微球的形态。通过差示扫描量热法(DSC)和 X 射线衍射研究药物与聚合物之间的相互作用。在含有 Pectinex Ultra SP-L 或 1%(w/v)大鼠盲肠内容物的模拟结肠液中进行体外药物释放研究,结果表明,在存在 1%(w/v)大鼠盲肠内容物的情况下,姜黄素的释放显著增加。可以得出结论,Eudragit® S100 包衣的果胶酸钙微球是姜黄素结肠传递的潜在载体。