7-乙基-10-羟基喜树碱白蛋白纳米粒的制备及其药动学与毒性的研究
Preparation,pharmacokinetics and toxicity studies of lipid albumin nanoparticle loaded with 7-ethyl-10-hydroxycamptothecin
作者:郑丹;刘欢;龚涛;张志荣;
Author:
收稿日期: 年卷(期)页码:2014,29(05):-497-499
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:7-乙基-10-羟基喜树碱;白蛋白纳米粒;药动学;骨髓抑制
Key words:
基金项目:
中文摘要
目的制备7-乙基-10-羟基喜树碱白蛋白纳米粒(SN38-HSA-LN)来延长药物在体内的循环时间并降低毒性。方法采用高压均质法制备SN38白蛋白纳米粒,并对制剂的形态学、粒径、包封率进行考查;同时采用LC-MS/MS法测定其在大鼠血浆中的药物浓度;并通过检测大鼠的外周血白细胞数量来评价其骨髓抑制毒性。结果制备的纳米粒大小均匀,形态良好,包封率为88.14%±3.15%,粒径为162.3±5.9 nm,PDI为0.137±0.015;大鼠尾静脉iv给药后,SN38-HSA-LN较SN38溶液的t1/2延长,AUC显著增加,且骨髓抑制程度明显降低。结论制备的SN38-HSA-LN包封率较高,粒径大小分布均匀,静脉注射延长了药物血液循环时间,并降低了骨髓抑制毒性。
参考文献
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