【摘要】 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。更多还原

【Abstract】 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 of 1 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.CONCLUSION Copolymer micelles could improve the lactone stability of 9-NC.更多还原