Abd-Elbary A, El-laithy H M, Tadros M I
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Int J Pharm. 2008 Jun 5;357(1-2):189-98. doi: 10.1016/j.ijpharm.2008.01.056. Epub 2008 Feb 7.
A Novel approach was developed for the preparation of controlled release proniosome-derived niosomes, using sucrose stearates as non-ionic biocompatible surfactants for the nebulisable delivery of cromolyn sodium. Conventional niosomes were prepared by a reverse phase evaporation method followed by the preparation of proniosomes by spraying the optimized surfactant-lipid mixture of sucrose stearate, cholesterol and stearylamine in 7:3:0.3 molar ratio onto the surface of spray dried lactose powder. Proniosome-derived niosomes were obtained by hydrating proniosomes with 0.9% saline at 50 degrees C and mixing for approximately 2 min. All vesicles were evaluated for their particle size, morphological characteristics, entrapment efficiency, in vitro drug release, nebulisation efficiency and physical stability at 2-8 degrees C. In addition, coating carrier surface with the surfactant-lipid mixture, during preparation of proniosomes, resulted in smaller, free flowing, homogenous and smooth vesicles with high drug entrapment efficiency. Compared to a standard drug solution, a successful retardation of the drug release rate was achieved with the proniosome-derived niosomes, where the t50% value of the release profile was 18.1h compared to 1.8h. Moreover, high nebulisation efficiency percentage and good physical stability were also achieved. The results are very encouraging and offer an alternative approach to minimize the problems associated with conventional niosomes like degradation, sedimentation, aggregation and fusion.
开发了一种制备控释前体脂质体衍生脂质体的新方法，使用蔗糖硬脂酸盐作为非离子生物相容性表面活性剂用于雾化递送色甘酸钠。通过反相蒸发法制备传统脂质体，然后通过将蔗糖硬脂酸盐、胆固醇和硬脂胺的摩尔比为7:3:0.3的优化表面活性剂-脂质混合物喷雾到喷雾干燥乳糖粉末表面来制备前体脂质体。通过在50℃下用0.9%盐水水合前体脂质体并混合约2分钟获得前体脂质体衍生脂质体。对所有囊泡进行粒径、形态特征、包封率、体外药物释放、雾化效率和2-8℃下的物理稳定性评估。此外，在前体脂质体制备过程中用表面活性剂-脂质混合物包被载体表面，得到了更小、自由流动、均匀且光滑的囊泡，具有高药物包封率。与标准药物溶液相比，前体脂质体衍生脂质体成功延缓了药物释放速率，其释放曲线的t50%值为18.1小时，而标准药物溶液为1.8小时。此外，还实现了高雾化效率百分比和良好的物理稳定性。结果非常令人鼓舞，为最小化与传统脂质体相关的降解、沉淀、聚集和融合等问题提供了一种替代方法。
