Zhang Shuisheng, Huang Can, Li Zhengzheng, Yang Yongjie, Bao Tingting, Chen Haibo, Zou Yinghua, Song Li
a Department of Interventional Radiology and Vascular Surgery , Peking University First Hospital , Beijing , China.
b Department of Radiology, Beijing Chaoyang Hospital , Capital Medical University , Beijing , China.
Drug Deliv. 2017 Nov;24(1):1011-1017. doi: 10.1080/10717544.2017.1344336.
CalliSpheres Beads (CB) is the first drug-eluting bead (DEB) product in China. Our aim was to compare the effect on the pharmacokinetics of doxorubicin (DOX) and its local concentration between lipiodol emulsions and CB in the process of TACE in rabbit livers. Twenty-five rabbits were distributed into two groups; Group 1 received lipiodol emulsions with DOX, and Group 2 received CB loaded with DOX (CBDOX). DOX was measured in the peripheral blood at different times after treatment. Livers were sampled at 1 week and 1 month for Group 2 after embolization. DOX concentration and distribution were measured in the liver. The administration of DOX by TACE with CBDOX resulted in peripheral blood DOX concentrations of 39.85 ± 13.86 ng/mL at 5 min, with a gradual decrease to 6.89 ± 1.62 ng/mL at 24 h, after treatment. Plasma concentration of DOX after chemoembolization with lipiodol was 225.91 ± 64.88 ng/mL at 5 min and decreased with time by 24 h to 5.06 ± 0.48 ng/mL. In CBDOX group, the drug impregnated an area as far as 200 μm from the bead edge. The tissue concentration of doxorubicin (tissC) ranged from 40.27 μg/mL to 245.70 μg/mL at 1 week and from 5.64 μg/mL to 28.09 μg/mL at 1 month. Plasma concentrations of DOX resulting from CBDOX embolization were significantly lower than that for cTACE. CB could deliver relatively high concentrations of DOX to an area as far as 200 μm from the bead edge for at least 1 month.
载药微球（CB）是中国首个药物洗脱微球（DEB）产品。我们的目的是比较碘油乳剂和CB在兔肝TACE过程中对阿霉素（DOX）药代动力学及其局部浓度的影响。25只兔子分为两组；第1组接受含DOX的碘油乳剂，第2组接受载有DOX的CB（CBDOX）。治疗后不同时间点检测外周血中的DOX。第2组在栓塞后1周和1个月取肝脏样本。检测肝脏中DOX的浓度和分布。用CBDOX进行TACE给药后，治疗后5分钟外周血DOX浓度为39.85±13.86 ng/mL，24小时逐渐降至6.89±1.62 ng/mL。碘油化疗栓塞后5分钟DOX血浆浓度为225.91±64.88 ng/mL，24小时随时间下降至5.06±0.48 ng/mL。在CBDOX组，药物浸渍到距微球边缘200μm的区域。阿霉素组织浓度（tissC）在1周时为40.27μg/mL至245.70μg/mL，1个月时为5.64μg/mL至28.09μg/mL。CBDOX栓塞导致的DOX血浆浓度显著低于cTACE。CB可将相对高浓度的DOX输送到距微球边缘至少200μm的区域至少1个月。
