Ohta S, Nitta N, Sonoda A, Seko A, Tanaka T, Takahashi M, Kimura Y, Tabata Y, Murata K
Department of Radiology, Shiga University of Medical Science, Seta Tsukinowa-cho, Otsu City, Shiga, Japan.
Br J Radiol. 2009 May;82(977):380-5. doi: 10.1259/bjr/27737783. Epub 2008 Dec 19.
The object of this study was to generate cisplatin-conjugated gelatin microspheres (GMSs) and to confirm the subsequent release of cisplatin in vitro. The GMSs (1 mg) were immersed in 50 microl of a cisplatin solution (0.06, 0.15, 0.27, 0.30 or 0.54 mg ml(-1)) at 38 degrees C to allow conjugation. The cisplatin-conjugated GMSs were then extensively washed in double-distilled water and freeze-dried. The platinum concentration in the GMSs samples was investigated as a function of the concentration of cisplatin solution used in their preparation, the number of immersions in cisplatin (1, 2, 3, 4 or 5) and the period of immersion (1, 6 or 11 h). In vitro release tests were performed at different time intervals (1, 3, 6, 12 or 24 h) to allow the rate of cisplatin release to be calculated. The platinum concentration of the GMSs increased in proportion to the concentration of cisplatin solution and the length or number of immersions in cisplatin. In vitro release tests demonstrate that the release rate (%) from GMSs after 1, 3, 6, 12 or 24 h was 4.8, 5.5, 7.6, 10.0 and 12.4, respectively. We demonstrated the ability of GMSs to bind cisplatin forming cisplatin-conjugated GMSs. Moreover, we showed that cisplatin continued to bind GMSs strongly during the in vitro release test.
本研究的目的是制备顺铂共轭明胶微球（GMSs）并确认顺铂随后在体外的释放情况。将GMSs（1毫克）于38摄氏度下浸入50微升顺铂溶液（0.06、0.15、0.27、0.30或0.54毫克/毫升）中以实现共轭。然后将顺铂共轭的GMSs在双蒸水中充分洗涤并冻干。研究了GMSs样品中铂的浓度与制备过程中所用顺铂溶液浓度、顺铂浸泡次数（1、2、3、4或5次）以及浸泡时间（1、6或11小时）之间的关系。在不同时间间隔（1、3、6、12或24小时）进行体外释放试验，以计算顺铂的释放速率。GMSs中铂的浓度与顺铂溶液的浓度以及顺铂浸泡的时间长度或次数成正比。体外释放试验表明，GMSs在1、3、6、12或24小时后的释放率（%）分别为4.8、5.5、7.6、10.0和12.4。我们证明了GMSs结合顺铂形成顺铂共轭GMSs的能力。此外，我们还表明在体外释放试验期间顺铂持续强烈地结合GMSs。
