Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Cairo, Egypt.
J Microencapsul. 2010;27(5):377-86. doi: 10.3109/02652040903243445.
The aim of this project was to develop and optimize indomethacin microcapsules composed of multiple mucoadhesive polymers for high drug entrapment, good mucoadhesiveness and drug release in a controlled fashion over a longer period of time. Microcapsules containing sodium alginate, sodium carboxymethylcellulose, methylcellulose, Carbopol 934 and hydroxypropyl methylcellulose were prepared by orifice-ionic gelation method. The effects of composition of microcapsules on drug entrapment efficacy, drug release and mucoadhesive character were determined by mixture statistical design. Most formulations exhibited good mucoadhesive property in everted intestinal sac test. Drug entrapment efficiency (68-94%) was dependent on the type of polymers. Drug release (92-100%) extended over 12 h. The optimized formulation resulted in drug entrapment efficiency of 89.3%, drug release of 94.8% and mucoadhesiveness of 30.4%. All formulations were stable for more than 1.5 years. The optimized mucoadhesive microcapsules are promising for controlled delivery of indomethacin with twice a day oral administration.
本项目旨在开发和优化由多种粘膜粘附聚合物组成的吲哚美辛微胶囊，以实现高药物包封率、良好的粘膜粘附性和更长时间的药物控释。通过孔-离子凝胶化法制备含有海藻酸钠、羧甲基纤维素钠、甲基纤维素、卡波姆 934 和羟丙基甲基纤维素的微胶囊。通过混合统计设计确定微胶囊的组成对药物包封效率、药物释放和粘膜粘附特性的影响。大多数制剂在肠囊外翻试验中表现出良好的粘膜粘附性。药物包封效率（68-94%）取决于聚合物的类型。药物释放（92-100%）持续超过 12 小时。优化的配方导致药物包封效率为 89.3%，药物释放为 94.8%，粘膜粘附性为 30.4%。所有配方在 1.5 年以上的时间内均稳定。优化的粘膜粘附性微胶囊有望用于控制吲哚美辛的递药，每天口服两次。
