Ilem-Ozdemir Derya, Gundogdu Evren, Ekinci Meliha, Ozgenc Emre, Asikoglu Makbule
a Department of Radiopharmacy, Faculty of Pharmacy , Ege University , Bornova, Izmir , Turkey.
Drug Dev Ind Pharm. 2015;41(9):1493-8. doi: 10.3109/03639045.2014.959022. Epub 2015 Jul 21.
The purpose of this work is to prepare a self-microemulsifying drug delivery system (SMEDDS) for risedronate sodium (RSD) and to compare the permeability with RSD solution. The solubility of RSD was determined in different vehicles. Phase diagrams were constructed to determine the optimum concentration of oil, surfactant, and cosurfactant. RSD SMEDDS was prepared by using a mixture of soybean oil, cremophor EL, span 80, and transcutol (2.02:7.72:23.27:61.74, w/w, respectively). The prepared RSD SMEDDS was characterized by droplet size value. In vitro Caco-2 cell permeability studies were performed for SMEDDS and solution of radioactive ((99 m)Tc-labeled RSD) and nonradioactive RSD. The experimental results indicated that RSD SMEDDS has good stability and its droplet size is between 216.68 ± 3.79 and 225.26 ± 7.65 during stability time. In addition, RSD SMEDDS has higher permeability value than the RSD solution for both radioactive and nonradioactive experiments. The results illustrated the potential use of SMEDDS for delivery of poorly absorbed RSD.
本研究旨在制备利塞膦酸钠（RSD）的自微乳化药物递送系统（SMEDDS），并与RSD溶液的渗透性进行比较。测定了RSD在不同载体中的溶解度。构建相图以确定油、表面活性剂和助表面活性剂的最佳浓度。采用大豆油、聚氧乙烯蓖麻油EL、司盘80和二乙二醇单乙基醚（比例分别为2.02:7.72:23.27:61.74，w/w）的混合物制备了RSD SMEDDS。通过液滴尺寸值对所制备的RSD SMEDDS进行表征。对SMEDDS以及放射性（（99m）Tc标记的RSD）和非放射性RSD的溶液进行了体外Caco-2细胞渗透性研究。实验结果表明，RSD SMEDDS具有良好的稳定性，在稳定期内其液滴尺寸在216.68±3.79至225.26±7.65之间。此外，在放射性和非放射性实验中，RSD SMEDDS的渗透性值均高于RSD溶液。结果表明SMEDDS在递送吸收不良的RSD方面具有潜在应用价值。
