Department of Diagnostic Radiology, The University of Texas M. D. Anderson Cancer Center, 1515 Holcombe Blvd, Houston, TX 77030, USA.
Cardiovasc Intervent Radiol. 2011 Oct;34(5):1021-30. doi: 10.1007/s00270-011-0154-6. Epub 2011 Apr 9.
The pharmacokinetic profile after hepatic arterial embolization with superabsorbent microspheres (QuadraSpheres) loaded with doxorubicin was studied.
Rabbits with hepatic VX2 tumors were treated with intra-arterial administration of QuadraSpheres loaded with doxorubicin, or transarterial chemoembolization (TACE) using doxorubicin, Lipiodol and Embospheres, or hepatic arterial infusion (HAI) of doxorubicin. Tumor specimens were evaluated by fluorescence microscopy, and plasma and tumor concentrations of doxorubicin were measured.
The peak plasma concentration of doxorubicin was lower in the QuadraSphere group (309.9 ng/ml) than in the HAI (673.4 ng/ml) or TACE (360.5 ng/ml) groups, suggesting higher tumor retention in the QuadraSphere group. Intratumoral doxorubicin levels declined to negligible levels at 1 and 3 days after treatment, respectively, in the HAI and TACE groups. In the QuadraSphere groups, intratumoral doxorubicin level declined after day 1, but was still detectable at 14 days after treatment and was higher than that in the other groups at 1, 3, and 7 days. Intratumoral doxorubicin fluorescence was detected at all time points in the QuadraSphere group, but only at 1 day after treatment in the TACE group.
Hepatic arterial administration of doxorubicin-loaded QuadraSpheres enables the sustained release of doxorubicin to hepatic tumors.
研究载多柔比星的超吸收微球（QuadraSpheres）经肝动脉栓塞后的药代动力学特征。
用载有阿霉素的 QuadraSpheres、阿霉素、碘油和 Embospheres 的经动脉化疗栓塞（TACE）或阿霉素肝动脉灌注（HAI）对荷 VX2 肿瘤兔进行经动脉给药。用荧光显微镜评估肿瘤标本，测量血浆和肿瘤中阿霉素的浓度。
载多柔比星的 QuadraSphere 组（309.9ng/ml）的血浆中多柔比星峰浓度低于 HAI 组（673.4ng/ml）或 TACE 组（360.5ng/ml），表明 QuadraSphere 组肿瘤内的保留率更高。HAI 和 TACE 组在治疗后第 1 和第 3 天，肿瘤内阿霉素水平分别降至可忽略水平。在 QuadraSphere 组中，肿瘤内阿霉素水平在第 1 天后下降，但在治疗后第 14 天仍可检测到，并且在第 1、3 和 7 天高于其他组。在 QuadraSphere 组中，在所有时间点均检测到肿瘤内阿霉素荧光，但在 TACE 组仅在治疗后第 1 天检测到。
肝动脉内给予载多柔比星的 QuadraSpheres 可使阿霉素持续释放到肝肿瘤中。
