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Study on oily drug carriers with blood-embolism potential

具有血液栓塞潜力的油性药物载体的研究

基本信息

批准号：
62570971
负责人：
SUGIBAYASHI Kenji
金额：
$ 1.15万
依托单位：
Josai University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1987
资助国家：
日本
起止时间：
1987 至 1988
项目状态：
已结题

项目摘要

Findings and results obtained for utilities of oily drug carriers with blood vessel-embolism capacity are follows:(1) Oleic acid (OA) and ethyl oleate (EO) were selected as oily drug carriers and aluminum stearate and ethyl cellulose were added to enhance the blood vesselembolism capacity to OA and EO, respectively.(2) Visual microscopical observation of blood vessel-embolism capacity after intra-arterial infusion in the cheek pouch in hamsters suggested that embolism periods and sites could be modified by changing the viscosity of the oily carriers.(3) Retainment of oils after intra-arterial infusion of viscous EO into the stomach, Kidney and liver in rats was increased by increasing the viscosity of the oily carriers. Percent retainment in the liver was most effective, followed by those in the stomach and kidney. When comparing viscous OA with viscous EO, the former showed higher retainment and was less safe.(4) Similar retainment experiments after infusing cisplatin-entrapped viscous EO in rats which AH 272 cells were inoculated showed that the viscous EO and entrapped cisplatin significantly concentrated in the tumor sites of the liver.(5) Cisplatin-entrapped viscous EO showed marked antitumor effect on the AH 272 bearing rats. The effects were higher than those of free cisplatin and cisplatin free viscous Eo. These results suggest that viscous oily drug carriers can be used as a targeted delivery system in cancer chemotherapy.

本文对具有血管栓塞能力的油性药物载体的应用进行了研究，结果如下：（1）选用油酸（OA）和油酸乙酯（EO）作为油性药物载体，分别加入硬脂酸铝和乙基纤维素，以增强OA和EO的血管栓塞能力。(2)通过对金黄地鼠颊囊动脉灌注后血管栓塞容量的肉眼显微镜观察，提示可通过改变油性载体的粘度来改变栓塞时间和栓塞部位。(3)通过增加油性载体的粘度，将粘性EO动脉内输注到大鼠胃、肾和肝中后，油的保留增加。肝脏中的保留百分比最有效，其次是胃和肾脏。当将粘性OA与粘性EO进行比较时，前者显示出更高的保持性，并且不太安全。(4)在接种AH 272细胞的大鼠中输注顺铂包封的粘性EO后的类似保留实验表明，粘性EO和顺铂包封的粘性EO显著地集中在肝脏的肿瘤部位。(5)载顺铂的粘性环氧乙烷对AH 272荷瘤大鼠有明显的抗肿瘤作用。其作用优于游离顺铂和游离顺铂的粘性Eo。这些结果表明，粘性油性药物载体可用作癌症化疗的靶向递送系统。