Lee D W, Hwang S J, Park J B, Park H J
Graduate School of Biotechnology, Korea University, Seoul 136-701, Korea.
J Microencapsul. 2003 Mar-Apr;20(2):179-92.
To prevent a rapid drug release from alginate microspheres in simulated intestinal media, alginate microspheres were coated or blended with polymers. Three polymers were selected and evaluated such as HPMC, Eudragit RS 30D and chitosan, as both coating materials and additive polymers for controlling the drug release. This study focused on the release characteristics of polymer-coated and blended alginate microspheres, varying the type of polymer and its concentration. The alginate microspheres were prepared by dropping the mixture of drug and sodium alginate into CaCl(2) solution using a spray-gun. Polymer-coated microspheres were prepared by adding alginate microspheres into polymer solution with mild stirring. Polymer-blended microspheres were prepared by dropping the mixture of drug, sodium alginate and additive polymer with plasticizer into CaCl(2) solution. In vitro release test was carried out to investigate the release profiles in 500 ml of phosphate buffered saline (PBS, pH 7.4). As the amount of polymer in sodium alginate or coating solution increase, the drug release generally decreased. HPMC-blended microspheres swelled but withstood the disintegration, showing an ideal linear release profiles. Chitosan-coated microspheres showed smooth and round surface and extended the release of drug. In comparison with chitosan-coated microspheres, HPMC-blended alginate microspheres can be easily made and used for controlled drug delivery systems due to convenient process and controlled drug release.
为防止藻酸盐微球在模拟肠道介质中快速释放药物,藻酸盐微球用聚合物进行了包衣或混合。选择并评估了三种聚合物,如羟丙甲纤维素(HPMC)、丙烯酸树脂Eudragit RS 30D和壳聚糖,作为控制药物释放的包衣材料和添加剂聚合物。本研究聚焦于聚合物包衣和混合的藻酸盐微球的释放特性,改变聚合物的类型及其浓度。藻酸盐微球通过用喷枪将药物和海藻酸钠的混合物滴入氯化钙溶液中制备。聚合物包衣微球通过将藻酸盐微球加入聚合物溶液中并轻轻搅拌来制备。聚合物混合微球通过将药物、海藻酸钠和添加剂聚合物与增塑剂的混合物滴入氯化钙溶液中制备。进行体外释放试验以研究在500毫升磷酸盐缓冲盐水(PBS,pH 7.4)中的释放曲线。随着海藻酸钠或包衣溶液中聚合物量的增加,药物释放通常会降低。HPMC混合微球膨胀但能耐受崩解,呈现出理想的线性释放曲线。壳聚糖包衣微球表面光滑且呈圆形,延长了药物释放。与壳聚糖包衣微球相比,HPMC混合藻酸盐微球由于制备过程简便且药物释放可控,易于制备并可用于控释给药系统。