Zhao Jun, Song Shaoli, Zhong Meng, Li Chun
Department of Experimental Diagnostic Imaging, The University of Texas MD Anderson Cancer Center, 1515 Holcombe Blvd., Houston, TX 77030, USA.
ACS Macro Lett. 2012 Jan 17;1(1):150-153. doi: 10.1021/mz200034f. Epub 2011 Dec 11.
We present a long-circulating biodegradable core-crosslinked polymeric micelle (d-CCPM) for the nuclear/optical imaging of tumors. The d-CCPM was derived from an amphiphilic block-copolymer consisting of a hydrophilic block of brush-like poly(ethylene glycol) and a hydrophobic block containing cleavable pendent triethoxysilane. The resultant imaging tracer had prolonged circulation in the blood (half-life of clearance phase = 36.5 hrs), substantial accumulation in tumor (% injected dose per gram of tissue = 8.5% ± 1.0% at 24 hrs post-injection) and minimal uptake in the liver (5.0% ± 0.1%) or spleen (5.1% ± 0.3%). Both nuclear and near-infrared fluorescence imaging revealed strong signals in tumor regions. At 48 hrs, nuclear imaging exhibited tumor-to-liver and tumor-to-blood ratios of 1.4 and 1.1, respectively. The degradation of d-CCPM was studied in vitro at pH 5.0 and 37°C; and confirmed by transmission electron microscopy confirmed. Our study indicates that the d-CCPM system is an effective probe for dual-modal cancer imaging and a potential safe platform nanocarrier for the delivery of anti-cancer drugs and cancer therapy.
我们展示了一种用于肿瘤核/光学成像的长循环可生物降解核交联聚合物胶束（d-CCPM）。d-CCPM由一种两亲性嵌段共聚物衍生而来，该共聚物由刷状聚乙二醇的亲水嵌段和含有可裂解侧基三乙氧基硅烷的疏水嵌段组成。所得的成像示踪剂在血液中循环时间延长（清除期半衰期 = 36.5小时），在肿瘤中大量积聚（注射后24小时每克组织的注射剂量百分比 = 8.5% ± 1.0%），在肝脏（5.0% ± 0.1%）或脾脏（5.1% ± 0.3%）中的摄取量最小。核成像和近红外荧光成像均显示肿瘤区域有强烈信号。在48小时时，核成像显示肿瘤与肝脏的比值为1.4，肿瘤与血液的比值为1.1。在pH 5.0和37°C条件下对d-CCPM的降解进行了体外研究；并通过透射电子显微镜得到证实。我们的研究表明，d-CCPM系统是一种用于双模态癌症成像的有效探针，也是一种用于递送抗癌药物和癌症治疗的潜在安全平台纳米载体。
