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针对目前化疗药物跨血脑屏障的能力差而导致对脑部神经胶质瘤治疗效果不佳的问题,该文拟制备偶联转铁蛋白以及氯毒素的双重脑靶向脂质体来突破这一障碍。研究双重脑靶向脂质体的处方、制备工艺并对其进行评价。采用反相蒸发法制备包载质粒的脂质体,以粒径和Zeta电位为评价指标进行处方筛选和工艺优化,采用柱层析法结合分光光度法分别测定包封率和偶联率,以动态光散射法对其粒径、Zeta电位等理化性质进行研究。结果:双重脑靶向脂质体的包封率为(90.0±5.1)%;转铁蛋白和氯毒素的偶联率分别为(41.5±6.1)%和(50.2±8.3)%;平均粒径为(219.9±7.4)nm,多分散指数(PDI)为0.216±0.038,Zeta电位值为(21.0±5.2)mV。反相蒸发法制备双重脑靶向脂质体工艺可行,且具有重现性好、包封率高、质量稳定等优点,预示着该给药系统可能具有良好的脑靶向性潜力,有助于解决传统化疗的局限问题。
In response to the current poor ability of chemotherapeutic drugs to cross the blood-brain barrier leading to poor response to brain glioma treatment, this paper intends to prepare dual-targeted targeting liposomes that conjugate transferrin and chlorotoxin to break through this An obstacle. The formulation of the dual brain targeted liposomes, the preparation process, and their evaluation were studied. Liposome encapsulated plasmids were prepared by reverse phase evaporation method. Prescriptions and process optimization were evaluated by particle size and Zeta potential. The entrapment efficiency and coupling efficiency were determined by column chromatography and spectrophotometry, respectively Dynamic light scattering method to study its particle size, Zeta potential and other physical and chemical properties. Results: The entrapment efficiency of double-brain targeted liposomes was (90.0 ± 5.1)% and that of transferrin and chlorotoxin was (41.5 ± 6.1) and (50.2 ± 8.3)%, respectively (219.9 ± 7.4) nm, the polydispersity index (PDI) was 0.216 ± 0.038 and the Zeta potential was (21.0 ± 5.2) mV. The reverse-phase evaporation method for the preparation of dual-brain targeting liposomes is feasible and reproducible, with high entrapment efficiency and stable quality, indicating that the drug delivery system may have good potential for brain targeting and is helpful To solve the limitations of traditional chemotherapy.