Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH-sensitive drug release property.
Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH-sensitive drug release property.
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DOI：
10.1016/j.colsurfb.2008.10.013
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发表时间：
2009-02
期刊：
影响因子：
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通讯作者：
Cui Yu;Bo-Cheng Yin;Wei Zhang-;Si-Xue Cheng;Xianzheng Zhang;R. Zhuo
中科院分区：
文献类型：
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作者：
Cui Yu;Bo-Cheng Yin;Wei Zhang-;Si-Xue Cheng;Xianzheng Zhang;R. Zhuo
以牛血清白蛋白(BSA)为模型药物，研制了以壳聚糖、海藻酸盐和果胶为基质的pH敏感性提高的蛋白质类药物复合微球给药系统。用一种简便的粉碎方法制备了平均粒径小于200μm的复合载药微球。由于微球是通过三聚磷酸盐的交联、海藻酸盐和/或果胶的静电络合以及与钙离子的电致凝胶形成的，所以微球具有更好的pH敏感性药物释放性能。在模拟胃(pH 1.2和pH 5.0)、肠道(pH 7.4)和结肠(pH 6.0和带酶pH 6.8)介质中考察了微球的体外释药行为。对于组成合适的复合微球，在pH 1.2和pH 5.0时，BSA能有效地被释放，而在pH 7.4，pH 6.8和pH 6.0时，BSA的释放显著增加，尤其是在果胶酶的存在下。这些结果清楚地表明，这些微粒具有通过口服给药的位置特异性蛋白药物的潜力。
Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH sensitivity were developed for oral delivery of protein drugs, using bovine serum albumin (BSA) as a model drug. The composite drug-loaded microparticles with a mean particle size less than 200μm were prepared by a convenient shredding method. Since the microparticles were formed by tripolyphosphate cross-linking, electrostatic complexation by alginate and/or pectin, as well as ionotropic gelation with calcium ions, the microparticles exhibited an improved pH-sensitive drug release property. The in vitro drug release behaviors of the microparticles were studied in simulated gastric (pH 1.2 and pH 5.0), intestinal (pH 7.4) and colonic (pH 6.0 and pH 6.8 with enzyme) media. For the composite microparticles with suitable compositions, the releases of BSA at pH 1.2 and pH 5.0 could be effectively sustained, while the releases at pH 7.4, pH 6.8 and pH 6.0 increased significantly, especially in the presence of pectinase. These results clearly suggested that the microparticles had potential for site-specific protein drug delivery through oral administration.