[摘要]：Nanoliposome can be designed as a drug delivery carrier to improve the pharmacological and therapeutic properties of drug administration. Re-188-labeled nanoliposomes are useful for diagnostic imaging as well as for targeted radionuclide therapy. In this study, the in vivo nuclear imaging, pharmacokinetics and biodistribution of administered nanoliposomes were investigated as drug and radionuclide carriers for targeting solid tumor via intravenous (i.v.) administration. The radiotherapeutics (Re-188-liposome) and radiochemotherapeutics (Re-188-DXR-liposome) were i.v. administered to nude mice bearing human HT-29 colorectal adenocarcinoma xenografits. Re-188-liposome and Re-188-DXR-liposoms show similar biodistribution profile; both have higher tumor uptake, higher blood retention time, and lower excretion rate than Re-188-N,N-bis(2-mercaptoethyl)-N',N'-diethylenediamine (BMEDA). In contrast to tumor uptake, the area under the curve (AUC) value of tumor for Re-188-liposome and Re-188-DXR-liposome was 16.5- and 11.5-fold higher than that of free Re-188-BMEDA, respectively. Additionally, Re-188-liposome and Re-188-DXR-liposome had a higher tumor-to-muscle ratio at 24 h (14.4 +/- 2.7 and 17.14 +/- 4.1, respectively) than Re-188-BMEDA (1.6 +/- 0.1). The tumor targeting and distribution of Re-188-(DXR)-liposome (representing Re-188-DXR-liposome and Re-188-liposome) can also be acquired by signal photon-emission computed tomography/computed tomography images as well as whole body autoradiograph. These results suggest that Re-188-(DXR)-liposomes are potentially promising agents for passive targeting treatment of malignant disease.
