Wada Masahiro, Jinno Hiromitsu, Ueda Masakazu, Ikeda Tadashi, Kitajima Masaki, Konno Tomohiro, Watanabe Junji, Ishihara Kazuhiko
Department of Surgery, Keio University School of Medicine, 35 Shinanomachi, Shinjuku-ku, Tokyo 160-8582, Japan.
Anticancer Res. 2007 May-Jun;27(3B):1431-5.
Paclitaxel (PTX) is administered as a solution in polyoxyethylated castor oil (CO) due to its low water solubility, but solvent-induced side-effects may be severe.
PMB30W is a co-polymer of 2-methacryloyloxyethyl phosphorylcholine (MPC) and butyl methacrylate (BMA). Cytotoxicities of PTX in PMB30W (PTX-PMB30W) were examined in cell culture and in vivo.
PTX-PMB30W and PTX in dimethyl sulfoxide showed similar toxicity in breast cancer cell lines MCF-7, SK-BR-3 and MX-1. Antitumor efficacies of PTX-PMB30W and PTX in CO (PTX-CO) were similar following weekly intraperitoneal administration of 50 mg/kg PTX in nude mice transplanted with MX-1 cells. At 200 mg/kg PTX, all animals died within 1 minute of PTX-CO administration. However, all animals receiving PTX-PBM30W survived. Ulceration occurred following subcutaneous injection of PTX-CO, but injection of PTX-PMB30W did not cause skin changes.
Our data suggest that PMB30W can act as an effective PTX nanotransporter.
由于紫杉醇（PTX）水溶性低，其以聚氧乙烯蓖麻油（CO）溶液形式给药，但溶剂诱导的副作用可能很严重。
PMB30W是2-甲基丙烯酰氧基乙基磷酰胆碱（MPC）和甲基丙烯酸丁酯（BMA）的共聚物。在细胞培养和体内研究了PTX在PMB30W（PTX-PMB30W）中的细胞毒性。
PTX-PMB30W和二甲基亚砜中的PTX在乳腺癌细胞系MCF-7、SK-BR-3和MX-1中显示出相似的毒性。在每周腹腔注射50mg/kg PTX的移植MX-1细胞的裸鼠中，PTX-PMB30W和CO中的PTX（PTX-CO）的抗肿瘤疗效相似。在PTX剂量为200mg/kg时，所有接受PTX-CO给药的动物在1分钟内死亡。然而，所有接受PTX-PBM30W的动物都存活下来。皮下注射PTX-CO后出现溃疡，但注射PTX-PMB30W未引起皮肤变化。
我们的数据表明，PMB30W可作为一种有效的PTX纳米转运体。
