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首页> 外文期刊>Drug Design, Development and Therapy >Targeting brain cells with glutathione-modulated nanoliposomes: in vitro and in vivo study
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Targeting brain cells with glutathione-modulated nanoliposomes: in vitro and in vivo study

机译：用谷胱甘肽调节的纳米脂质体靶向脑细胞：体外和体内研究

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Background: The blood–brain barrier prevents many drug moieties from reaching the central nervous system. Therefore, glutathione-modulated nanoliposomes have been engineered to enhance the targeting of flucytosine to the brain. Methods: Glutathione-modulated nanoliposomes were prepared by thin-film hydration technique and evaluated in the primary brain cells of rats. Lecithin, cholesterol, and span 65 were mixed at 1:1:1 molar ratio. The molar percentage of PEGylated glutathione varied from 0?mol% to 0.75?mol%. The cellular binding and the uptake of the targeted liposomes were both monitored by epifluorescent microscope and flow cytometry techniques. A biodistribution and a pharmacokinetic study of flucytosine and flucytosine-loaded glutathione–modulated liposomes was carried out to evaluate the in vivo brain-targeting efficiency. Results: The size of glutathione-modulated nanoliposomes was <100?nm and the zeta potential was more than -65 mV. The cumulative release reached 70% for certain formulations. The cellular uptake increased as molar percent of glutathione increased to reach the maximum at 0.75?mol%. The uptake of the targeted liposomes by brain cells of the rats was three times greater than that of the nontargeted liposomes. An in vivo study showed that the relative efficiency was 2.632±0.089 and the concentration efficiency was 1.590±0.049, and also, the drug-targeting index was 3.670±0.824. Conclusion: Overall, these results revealed that glutathione-PEGylated nanoliposomes enhance the effective delivery of flucytosine to brain and could become a promising new therapeutic option for the treatment of the brain infections.
机译：背景：血脑屏障可阻止许多药物部分到达中枢神经系统。因此，已经设计了谷胱甘肽调节的纳米脂质体以增强氟胞嘧啶对大脑的靶向。方法：采用薄膜水化技术制备谷胱甘肽调节的纳米脂质体，并在大鼠原代脑细胞中进行评价。卵磷脂，胆固醇和跨度65以1：1：1的摩尔比混合。聚乙二醇化谷胱甘肽的摩尔百分比在0？mol％至0.75？mol％之间变化。细胞结合和靶向脂质体的摄取均通过落射荧光显微镜和流式细胞术技术监测。对氟胞嘧啶和载有氟胞嘧啶的谷胱甘肽调节脂质体进行了生物分布和药代动力学研究，以评估体内脑靶向效率。结果：谷胱甘肽调节的纳米脂质体的大小小于100？nm，ζ电位大于-65 mV。某些制剂的累积释放达到70％。随着谷胱甘肽摩尔百分比的增加，细胞摄取增加，达到最大浓度0.75？mol％。大鼠脑细胞对目标脂质体的吸收是非目标脂质体的三倍。体内研究表明，相对效率为2.632±0.089，浓缩效率为1.590±0.049，而且药物靶向指数为3.670±0.824。结论：总体而言，这些结果表明谷胱甘肽-聚乙二醇化纳米脂质体可增强氟胞嘧啶向大脑的有效递送，并可能成为治疗脑部感染的有希望的新治疗选择。

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