Development of intelligent-type drug delivery system by transporter protein.

我们合成了NGR (Asn-Gly-Arg)-lipocalin-type prostaglandin D synthase (L-PGDS)，具有肿瘤靶向的NGR基序，特异性结合在血管生成血管内皮中表达的CD13受体。NGR-L-PGDS与难水溶性抗肿瘤药物SN-38络合。2 mM NGR-L-PGDS存在时SN-38在PBS中的溶解度比在PBS中的溶解度提高了300倍。与对照组相比，静脉给药SN-38/NGR-L-PGDS复合物显著抑制人结肠癌小鼠异种移植肿瘤模型的肿瘤生长。

We generated NGR (Asn-Gly-Arg)-lipocalin-type prostaglandin D synthase (L-PGDS), possessing tumor-targeting NGR-motif, which specifically binds to CD13 receptor expressing in the endothelium of angiogenic blood vessels. NGR-L-PGDS was complexed with SN-38 which is a poorly water-soluble antitumor drug. The solubility of SN-38 in the presence of 2 mM NGR-L-PGDS in PBS increased by 300-fold as compared with that in PBS. Intravenous administration of SN-38/NGR-L-PGDS complex dominantly inhibited tumor growth as compared with control in mouse xenograft tumor model using human colon cancer cells.