Department of Medical Biochemistry and Global COE Program, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Cancer Lett. 2010 Jan 28;287(2):165-71. doi: 10.1016/j.canlet.2009.06.008. Epub 2009 Jul 17.
Dual-targeting liposomes modified with Ala-Pro-Arg-Pro-Gly (APRPG) and Gly-Asn-Gly-Arg-Gly (GNGRG) peptides were developed. They remarkably associated to growing human umbilical vein endothelial cells (HUVECs) compared with single-targeting liposomes modified with APRPG or GNGRG. Doxorubicin (DOX) encapsulated in the dual-targeting liposomes significantly suppressed the growth of HUVECs compared with that in single-targeting liposomes. The dual-targeting liposomes containing DOX strongly suppressed tumor growth in Colon26 NL-17 carcinoma-bearing mice. Confocal microscopic data indicated that this anticancer effect was brought by the association of these liposomes to angiogenic vessels in the tumor. These findings suggest that "dual-targeting" would be a hopeful method for targeting therapies.
研制了同时被 Ala-Pro-Arg-Pro-Gly（APRPG）和 Gly-Asn-Gly-Arg-Gly（GNGRG）肽修饰的双靶向脂质体。与单独用 APRPG 或 GNGRG 修饰的靶向脂质体相比，它们与生长中的人脐静脉内皮细胞（HUVEC）显著结合。与单靶向脂质体相比，包封在双靶向脂质体中的阿霉素（DOX）显著抑制了 HUVEC 的生长。载有 DOX 的双靶向脂质体强烈抑制了携带 Colon26 NL-17 癌的小鼠的肿瘤生长。共聚焦显微镜数据表明，这种抗癌作用是通过这些脂质体与肿瘤中血管生成血管的结合产生的。这些发现表明，“双靶向”可能是一种有希望的靶向治疗方法。
