P. G. Department of Pharmaceutics, College of Pharmaceutical Sciences, Berhampur-760002 Orissa, India.
Acta Pharm. 2010 Sep;60(3):255-66. doi: 10.2478/v10007-010-0026-7.
Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.
离子凝胶作用被用于将双氯芬酸包埋到藻酸-果胶生物黏附性微球中,作为一种潜在的载药系统,用于将这种抗炎药物经口递送给患者。对微球进行了体外考察,以评估其是否具有潜在的持续释药性能,并考察其在体内作为双氯芬酸的胃保护系统的用途。分析了聚合物浓度和聚合物/药物的比例对微球性质的影响。微球表现出良好的生物黏附性,并且显示出较高的药物包封效率。药物释放曲线显示,双氯芬酸钠从藻酸盐微球中更快地释放,而藻酸-果胶微球则显示出延长的释放。Dunnett 多重比较分析表明,与纯药物相比,优化配方的足爪肿胀抑制百分比有显著差异。结论是,藻酸-果胶生物黏附性制剂表现出作为双氯芬酸钠的持续释放剂型的有前途的性质,并且在胃中提供了明显的组织保护。