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以Pluronic P123与F127(质量比2∶1)为载体,采用薄膜水化法制备包载抗癫痫药拉莫三嗪(lamotrigine,1)的混合胶束(PF胶束)并表征。结果显示PF混合胶束包封率为92.39%、载药量为4.88%、平均粒径为21.32 nm。与P123胶束相比,PF混合胶束显著改善了体系稳定性。细胞激光共聚焦图像显示,与游离罗丹明123(一种P-糖蛋白底物,2)相比,PF胶束可显著促进脑微血管内皮细胞对2的摄取。结果预示包载1的PF混合胶束有望成为治疗难治性癫痫的新型药物载体。
Pluronic P123 and F127 (mass ratio 2: 1) were used as carriers to prepare and characterize the mixed micelles (PF micelles) containing lamotrigine (1) as antiepileptic drug using membrane hydration method. The results showed that the encapsulation efficiency of PF mixed micelles was 92.39%, the drug loading was 4.88% and the average particle size was 21.32 nm. Compared with P123 micelles, PF mixed micelles significantly improve the stability of the system. Laser confocal laser imaging showed that PF micelles significantly promoted the uptake of 2 by brain microvascular endothelial cells compared to free rhodamine 123 (a P-glycoprotein substrate, 2). The results indicate that the PF mixed micelles loaded 1 is expected to become a new drug carrier for the treatment of refractory epilepsy.