In Vitro Characterization of Cisplatin-loaded Superabsorbent Polymer Microspheres Designed for Chemoembolization
In Vitro Characterization of Cisplatin-loaded Superabsorbent Polymer Microspheres Designed for Chemoembolization
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DOI：
10.1016/j.jvir.2010.02.009
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发表时间：
2010-06-01
影响因子：
2.9
通讯作者：
Nakamura, Hironobu
中科院分区：
文献类型：
--
作者：
Maeda, Noboru;Osuga, Keigo;Nakamura, Hironobu
目的：寻找合适的造影剂将顺铂负载到高吸水性树脂中，并分析顺铂在高吸水性树脂中的吸收和洗脱动力学。材料与方法：对一种新型高可溶性顺铂粉末的3种造影剂--碘沙酸320 mg/m L、碘海醇300 mg/m L和异丙咪醇300 m g/m L进行了溶解度测定。根据顺铂在每种造影剂中的溶解度预先确定合适的顺铂浓度。对于每个浓度，我们用原子吸收光谱仪评估顺铂的洗脱动力学。结果：药物洗脱前、后顺铂浓度分别为2.5 mg/mL、2.5 mg/mL、5.0 mg/mL。在这些浓度下，100 mg的SAP分别携带5 mg、25 mg和50 mg的顺铂，分别溶于异烟酸(2.5 mg/m L)和碘海醇(2.5 mg/m l和5.0 m g/m L)。载顺铂的SAP在氧乙酸和碘海醇中表现出相似的洗脱曲线，顺铂在1、3、6和24小时的洗脱分数分别为15%、40%、70%和95%。药物洗脱实验表明，顺铂在2.5 mg/m L异沙比酸溶液中平均粒径为0.31~0.61 mm，在2.5 mg/m l碘海醇溶液中为0.54~0.60 mm，在5.0 mg/m l碘海醇溶液中为0.63~0.59 mm。当与碘海醇混合时，SAP携带的顺铂剂量是与异沙比酸混合时的十倍，扩张幅度是异沙比酸的两倍。顺铂载药SAP有望成为临床治疗肝肿瘤的药物输送系统。
PURPOSE: To find appropriate contrast media to load cisplatin into superabsorbent polymer (SAP) and to analyze the absorption and elution kinetics of cisplatin to and from SAP.MATERIALS AND METHODS: Three contrast media-ioxaglic acid 320 mg/mL, iohexol 300 mg/mL, and iopamidol 300 mg/mL-were tested for solubility of a new highly soluble cisplatin powder. The appropriate concentrations of cisplatin were predetermined according to the solubility in each contrast medium. For each concentration, we assessed the cisplatin elution kinetics with an atomic absorption spectrophotometer. The SAP particle diameters (106-150 mu m dry size) before and after drug elution were also measured.RESULTS: The concentrations of cisplatin were predetermined as 2.5 mg/mL in ioxaglic acid, 2.5 mg/mL in iohexol, and 5.0 mg/mL in iohexol. At these concentrations, 100 mg of SAP carried 5 mg, 25 mg, and 50 mg of cisplatin dissolved in ioxaglic acid (2.5 mg/mL) and iohexol (2.5 mg/mL and 5.0 mg/mL), respectively. Cisplatin-loaded SAP in ioxaglic acid and iohexol exhibited similar elution profiles, with cisplatin fractions of 15%, 40%, 70%, and 95% at 1, 3, 6, and 24 hours, respectively. By drug elution, the mean particle diameter changed from 0.31 mm to 0.61 mm in ioxaglic acid (2.5 mg/mL), from 0.54 mm to 0.60 mm in iohexol 2.5 mg/mL, and from 0.63 mm to 0.59 mm in iohexol 5.0 mg/mL.CONCLUSIONS: SAP was confirmed to absorb and elute cisplatin within 24 hours. When mixed with iohexol, SAP carried a ten times larger dose of cisplatin and expanded twice as large as when mixed with ioxaglic acid. Cisplatin-loaded SAP may have potential as a drug delivery system for the clinical treatment of liver tumors.