Background: Drug delivery to the brain tumor is limited due to the presence of the blood-brain barrier (BBB).

Objective: This study aimed to evaluate the therapeutic effects of cisplatin-loaded PEGylated liposomes, targeted with the OX26 antibody (targeted liposomal cisplatin) against transferrin receptor expressing rat glioma C6 cells in vitro.

Methods: The liposomes were synthesized using reverse phase evaporation method and were conjugated to the OX26 monoclonal antibody. They were characterized in terms of size, drug encapsulation efficiency, morphology and drug release experiments using dynamic light scattering, atomic absorption spectrometry, scanning electron microscopy, and dialysis membrane methods. Then, their biological activities were evaluated on targeting the BBB.

Results and Discussion: The characterization results showed that spherical nanodrug with a size of 157 nm and drug loading efficiency of 24% was synthesized, which released 64% of the loaded cisplatin after 72 h in a controlled release manner. The nanoparticles caused an increase in the cisplatin cytotoxicity effects by 1.7-, 1.8- and 1.8-fold, compared to cisplatin-loaded PEGylated liposomes (liposomal cisplatin) after 24, 48 and 72h incubation, respectively against C6 cells. Moreover, targeted liposomal cisplatin showed promising results in the transport of cisplatin across the BBB, in which it caused an increase in the cisplatin cytotoxicity on C6 cells by 2.7- and 2.4-fold, compared to cisplatin and liposomal cisplatin, respectively.

Conclusion: Regarding the properties of the targeted liposomal cisplatin, it suggests that the potency of the formulation, to be evaluated, for the transport of cisplatin across the BBB, delivers it to the brain tumor in vivo.

中文翻译：

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OX26修饰的脂质体顺铂靶向的胶质瘤细胞的体外特征

背景：由于存在血脑屏障（BBB），限制了向脑肿瘤的药物输送。

目的：本研究旨在评估以OX26抗体（靶向脂质体顺铂）为靶标的顺铂加载的聚乙二醇化脂质体对表达转铁蛋白受体的大鼠神经胶质瘤C6细胞的体外治疗效果。

方法：采用反相蒸发法合成脂质体，并与OX26单克隆抗体结合。通过尺寸，药物包封效率，形态和药物释放实验，使用动态光散射，原子吸收光谱，扫描电子显微镜和透析膜方法对它们进行了表征。然后，针对BBB评估其生物学活性。

结果与讨论：表征结果表明，合成的球形纳米药物大小为157 nm，载药效率为24％，在72 h后以控释方式释放了64％的顺铂载药量。与分别加载C24细胞24、48和72h后，与负载顺铂的PEG化脂质体（顺铂脂质体）相比，纳米颗粒引起的顺铂细胞毒性作用提高了1.7、1.8和1.8倍。此外，靶向的脂质体顺铂在顺铂穿过BBB的转运中显示出可喜的结果，与顺铂和脂质体顺铂相比，顺铂对C6细胞的细胞毒性增加了2.7和2.4倍。

结论：关于靶向的脂质体顺铂的性质，这表明该待评估制剂对顺铂跨过血脑屏障的转运能力在体内将其递送至脑肿瘤。