共聚物胶束对硝基喜树碱内酯环稳定性的影响

Effect of copolymer micelles on lactone stability of 9-nitro-20(S)-camptothecin

目的评价共聚物胶束对9-硝基喜树碱(9-NC)内酯环稳定性的影响。方法采用HPLC法测定,以甲醇-PBS(70:30,pH6.5)为流动相,检测波长370 nm,流速1 ml.min-1。结果内酯和羧酸盐形式的9-NC能完全分离;在PBS(pH7.4)中培养160 min后,载药胶束中具有抗肿瘤活性的9-NC内酯比例占80%,而无胶束包覆的原料药中内酯比例仅15%。结论共聚物胶束能有效提高9-NC内酯环结构的稳定性。

OBJECTIVE To evaluate the effect of copolymer micelles on lactone stability of 9 - nitro - 20 （S） - camptothecin （9 - NC）. METHODS The detection was carried out with HPLC at 370 nm ; the mobile phase was consisted of methanol and phosphate buffer solution （PBS） （70 ： 30, pH6.5） with the flow rate ofl ml·min^-1.RESULTS The lactone form and carboxylate form of 9- NC could be separated completely. The linear range of two forms was 0. 2 - 10. 0 μg·ml^-1. After incubation in PBS （pH7. 4） for 160 min, 80 percent of 9 -NC in micelles were lactone form with high anticancer activity while 15 percent in free form of 9 -NC. CON- CLUSION Copolymer micelles could improve the lactone stability of 9 - NC.