Study on oily drug carriers with blood-embolism potential

具有血管栓塞力的油性药物载体的应用研究结果如下：(1)选择油酸(OA)和油酸乙酯(EO)作为油性药物载体，添加硬脂酸铝和乙基纤维素分别增强其对OA和EO的血管栓塞性。(2)动脉内注入金黄地鼠颊囊后血管栓塞量的视觉显微镜观察表明，通过改变油性载体的粘度可以改变栓塞期和栓塞点。(3)动脉内注入粘性EO后胃内保留油脂。增加油性载体的粘度，可增加大鼠的肾脏和肝脏。在肝脏中的保留百分比是最有效的，其次是胃和肾脏。(4)在接种AH272细胞的大鼠体内，注射顺铂包裹的黏性EO后，黏性EO和包裹顺铂的EO明显聚集在肝脏的肿瘤部位。(5)顺铂包裹的黏性EO对AH272荷瘤大鼠有明显的抗肿瘤作用。其疗效优于游离顺铂和无顺铂粘稠型EO。这些结果表明，粘性油性药物载体可作为肿瘤化疗的靶向给药系统。

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.