Department of Radiology, Shiga University of Medical Science, Setatsukinowa-cho, Otsu, Shiga, 520-2192, Japan.
Int J Nanomedicine. 2010 Aug 9;5:499-504. doi: 10.2147/ijn.s10944.
We developed a dextran-magnetite conjugated cisplatin (DM-Cis) complex for use in thermal ablation and as a chemotherapeutic drug. To produce DM-Cis we reacted Cis with 1 mL DM (56 mg/mL iron). The temperature rise of DM-Cis was measured in vitro and in vivo under a portable induction-heating (IH) device. Platinum desorption from DM-Cis over 24 hours was measured in bovine serum. In in vivo accumulation and magnet and exothermic experiments we used four rat groups. In group 1 we delivered DM-Cis intraperitoneally (ip) and placed magnets subcutaneously (sc). In group 2 we injected saline (ip) and placed magnets (sc). In group 3 we injected DM-Cis (ip) and placed a sc incision (sham). The control (group 4) received an ip injection of saline. Rectus abdominis muscle tissue was stained with hematoxylin-eosin and iron-stained tissue areas (μm(2)) were calculated. The maximum platinum concentration in DM-Cis was approximately 105.6 μg/mL. Over 24 hours, 33.48% of platinum from DM-Cis was released. There was a significant difference (P < 0.05) in the iron-stained area between group 1 and the other groups. The temperature in muscle tissue registered a maximum of 56°C after about 4 min. DM-Cis may represent a magnetically-accumulated anticancer drug with hyperthermic effects.
我们研发了一种葡聚糖-磁铁矿结合顺铂(DM-Cis)复合物,用于热消融和化疗药物。为了制备 DM-Cis,我们将 Cis 与 1 毫升 DM(56mg/mL 铁)反应。在便携式感应加热(IH)设备下,我们在体外和体内测量了 DM-Cis 的升温。在牛血清中测量了 DM-Cis 中铂在 24 小时内的解吸情况。在体内积累、磁体和放热实验中,我们使用了四组大鼠。在第 1 组中,我们将 DM-Cis 腹膜内(ip)给药,并在皮下(sc)放置磁铁。在第 2 组中,我们注射生理盐水(ip)并放置磁铁(sc)。在第 3 组中,我们注射 DM-Cis(ip)并在皮下切口(sham)处放置磁铁。对照组(第 4 组)接受 ip 生理盐水注射。用苏木精-伊红染色直肠腹直肌组织,并计算铁染色组织面积(μm²)。DM-Cis 中的最大铂浓度约为 105.6μg/mL。在 24 小时内,DM-Cis 中释放了 33.48%的铂。第 1 组与其他组之间的铁染色区域有显著差异(P<0.05)。肌肉组织中的温度在大约 4 分钟后达到最高 56°C。DM-Cis 可能代表一种具有高热效应的磁性积累抗癌药物。