二氢卟吩e6在艾氏荷瘤小鼠体内的分布

目的研究二氢卟吩e6(Ce6)在移植瘤小鼠体内吸收、分布及代谢的动态变化,以期为声动力疗法处理不同部位肿瘤的时间点提供科学依据。方法艾氏移植瘤小鼠尾静脉注射Ce6后,利用荧光分光光度法和小动物活体成像技术测定Ce6在小鼠不同组织的富集分布变化规律。结果小鼠尾静脉给药后,Ce6迅速分布于全身各组织,在2 h内,各组织药物浓度均达到峰值,其中以肝含量最高。随后各组织中药物浓度均开始下降,以肝中清除速度最快。肿瘤组织中的Ce6含量在注射后不断上升,2 h时达到最高,随后开始下降,2～10 h代谢比较缓慢,24 h时浓度降至最低,但仍高于其他组织。结论 Ce6在艾氏移植瘤中具有肿瘤组织选择性好、潴留时间长并可迅速从体内排出等优点,有着很好的临床应用前景,同时提出了不同组织类型不同部位的肿瘤应根据各自适当的时间点进行处理。

Chlorin e6 distribution in the Ehrlich ascites tumor-bearing mice

Objective To study the absorption,clearance and other pharmacokinetic characteristics of chlorin e6,and to provide a scientific basis for sonodynamic therapy （SDT） of tumors. Methods Erlich ascites tumor （EAT） cells were inoculated into mice,and the tumor-bearing mice received intravenous injection of Ce6 in a dose of 25 mg /kg. The distribution of Chlorin e6 （Ce6） in the tumor was observed by in vivo imaging techniques at 0. 5,1,2,4,6,8,10,12,18 and 24 h after injection. The mice were killed at 24 h after injection and the drug concenttrations in the tumor and different organ tissues were determined by spectrofluorophotometry. Results After intravenous injection,the Ce6 in the tissues increased to a peak value within two hours,and the highest concentration occurred in the liver. After 2 h the Ce6 level began to decrease with the time course. The concentration of Ce6 in the tumor began to increase after injection and reached the highest level at 2 hours after injection. Then it began to slowly decrease. Its metabolic activity was slow between 2-10 h,showing a retention in the tumor,and reached a minimum at 24 h,but still higher than that in other organs. Conclusions The Ce6 in the EAT tumor-bearing mice has a longer retention and selectivity in the tumor,can be cleared quickly from normal tissues,therefore,is promising for clinical application. According to different metabolic rates in different organs,tumors of different histological types and at different sites should be treated at appropriate time,respectively.