Pimm M V, Perkins A C, Duncan R, Ulbrich K
Cancer Research Campaign Laboratories, University of Nottingham, UK.
J Drug Target. 1993;1(2):125-31. doi: 10.3109/10611869308996068.
N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing doxorubicin and galactosamine have been developed to target the hepatocyte galactose receptor with the aim of organ-specific chemotherapy of primary and metastatic liver disease. Previous biodistribution studies in rats and mice have used tyrosinamide incorporated into the copolymer structure to permit labelling with 125I, enabling quantification of polymer distribution by dissection analysis. Radiolabelling of this copolymer with 131I, a radionuclide suitable for gamma scintigraphy, and the imaging analysis of its biodistribution in mice are reported. The present studies are the first to confirm the feasibility of imaging HPMA copolymer biodistribution, and such gamma scintigraphy will be of great value for clinical pharmacokinetic studies with this compound. Gamma scintigraphy is virtually the only non-invasive method of assessing hepatic uptake of this and similar materials.
已研发出含有阿霉素和半乳糖胺的N-(2-羟丙基)甲基丙烯酰胺(HPMA)共聚物，以靶向肝细胞半乳糖受体，用于原发性和转移性肝病的器官特异性化疗。此前在大鼠和小鼠身上进行的生物分布研究使用了掺入共聚物结构中的酪氨酰胺，以便用125I进行标记，从而通过解剖分析对聚合物分布进行定量。本文报道了用适合γ闪烁显像的放射性核素131I对该共聚物进行放射性标记，以及对其在小鼠体内生物分布的显像分析。本研究首次证实了对HPMA共聚物生物分布进行显像的可行性，这种γ闪烁显像对于该化合物的临床药代动力学研究具有重要价值。γ闪烁显像实际上是评估该物质及类似物质肝摄取的唯一非侵入性方法。
