The central nervous system has been identified as an anatomical reservoir for HIV due the difficulties in delivering therapeutic agents into the brain and this complication results in HIV-associated neurocognitive disorder that persists in infected patients. The brain regions that are potentially exposed to tissue deficits due to HIV have been reported in previous reports; therefore, it is important to determine the drugs that can enter and localize in brain regions that are known to be susceptible to HIV neurodegeneration. Sprague-Dawley rats received intraperitoneal doses of zidovudine and lamivudine (50 mg kg-1). Mass spectrometry methods were used to determine the pharmacokinetics, of zidovudine and lamivudine, in the brain using liquid chromatography tandem mass spectrometry and mass spectrometry imaging (MSI), respectively. Zidovudine and lamivudine displayed complementary pharmacokinetic curves indicating a rapid absorption and blood-brain barrier penetration of both drugs reaching Cmax at 0.5 h after single dose. MSI of coronal brain sections showed that zidovudine and lamivudine are mostly distributed in corpus callosum, globus pallidus, striatum, and the neocortex region. Mass spectrometry techniques were used to demonstrate that zidovudine and lamivudine drugs are able to reach and localize in brain regions that are targets of HIV neurodegeneration in the brain.

中文翻译：

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齐多夫定和拉米夫定作为与HIV相关的神经认知障碍的潜在治疗剂。

由于难以将治疗剂输送到大脑中，中枢神经系统已被确定为HIV的解剖库，这种并发症导致HIV相关的神经认知障碍在感染患者中持续存在。在先前的报道中已经报道了由于艾滋病毒可能暴露于组织缺陷的大脑区域。因此，重要的是确定可以进入并定位在已知易感染HIV神经变性的大脑区域的药物。Sprague-Dawley大鼠接受腹膜内注射齐多夫定和拉米夫定（50 mg kg-1）。分别使用液相色谱串联质谱法和质谱成像（MSI）质谱法分别测定齐多夫定和拉米夫定在大脑中的药代动力学。齐多夫定和拉米夫定显示出互补的药代动力学曲线，表明两种药物在单次给药后0.5 h达到Cmax时均迅速吸收并血脑屏障穿透。冠状脑切片的MSI显示齐多夫定和拉米夫定主要分布在call体，苍白球，纹状体和新皮层区域。质谱技术用于证明齐多夫定和拉米夫定药物能够到达并定位于大脑区域，该区域是大脑中HIV神经变性的靶标。纹状体和新皮质区。质谱技术用于证明齐多夫定和拉米夫定药物能够到达并定位于大脑区域，该区域是大脑中HIV神经变性的靶标。纹状体和新皮质区。质谱技术用于证明齐多夫定和拉米夫定药物能够到达并定位于大脑区域，该区域是大脑中HIV神经变性的靶标。