Doi K, Oku N, Toyota T, Shuto S, Sakai A, Itoh H, Okada S
Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Biol Pharm Bull. 1994 Oct;17(10):1414-6. doi: 10.1248/bpb.17.1414.
Reticuloendothelial system (RES)-avoiding liposomes are known to accumulate in tumor tissues due to passive targeting. Dipalmitoylphosphatidylfluorouridine (DPPF), a potent antitumor agent readily incorporated into the lipid bilayer, was embedded in RES-avoiding liposomes modified with a uronic acid derivative, palmityl-D-glucuronide (PGlcUA). The therapeutic effect of DPPF in PGlcUA-liposomes was examined in tumor-bearing mice. Free or liposomal DPPF was injected intravenously into BALB/c mice bearing subcutaneously implanted Meth A sarcomas. The RES-avoiding liposomal formulation using PGlcUA was effective in reducing tumors, and prolonging survival time compared with free DPPF and also DPPF in conventional liposomes. Therefore, PGlcUA-liposomes might be of practical use as drug carriers for anticancer agents, especially their derivatives for embedding in liposomal membranes.
已知可避开网状内皮系统（RES）的脂质体由于被动靶向作用而在肿瘤组织中蓄积。二棕榈酰磷脂酰氟尿苷（DPPF）是一种易于掺入脂质双层的强效抗肿瘤剂，它被包封于用糖醛酸衍生物棕榈酰-D-葡糖醛酸（PGlcUA）修饰的可避开RES的脂质体中。在荷瘤小鼠中检测了DPPF在PGlcUA脂质体中的治疗效果。将游离的或脂质体形式的DPPF静脉注射到皮下植入了Meth A肉瘤的BALB/c小鼠体内。与游离DPPF以及常规脂质体中的DPPF相比，使用PGlcUA的可避开RES的脂质体制剂在缩小肿瘤和延长生存时间方面有效。因此，PGlcUA脂质体作为抗癌剂的药物载体可能具有实际应用价值，尤其是其用于包埋在脂质体膜中的衍生物。
