As the HIV epidemic continues to contribute to global morbidity and mortality, the prevalence of HIV-associated neurological disorders (HAND) also continues to be a major concern in infected individuals, despite the widespread use of combination antiretroviral therapy. Therefore, current antiretroviral drugs should be able to reach therapeutic levels in the brain for the treatment of HAND. The brain distribution of the next-generation non-nucleoside reverse transcriptase inhibitor, rilpivirine (RPV) was investigated in healthy female Sprague–Dawley (SD) rats. The presented study involves the use of liquid chromatography-tandem mass spectrometry (LC–MS/MS) to estimate the concentrations of RPV in plasma and brain homogenate samples. The use of matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) provided regional spatial distribution of RPV in brain tissue sections. The localization of RPV was found to be relatively high in the hypothalamus, thalamus and corpus callosum, brain regions known to be associated with neurodegeneration during HAND (including the cerebral cortex). This study has shown that RPV has an excellent blood–brain barrier penetrability. Thus, in combination with other antiretroviral drugs, better central nervous system (CNS) protection against HAND can possibly be achieved.

中文翻译：

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Rilpivirine作为治疗HIV相关神经认知障碍（HAND）的潜在候选人。

随着艾滋病的流行继续加剧全球发病率和死亡率，尽管广泛使用联合抗逆转录病毒疗法，但与艾滋病毒相关的神经系统疾病（HAND）的患病率仍然是受感染个体的主要关注点。因此，当前的抗逆转录病毒药物应该能够达到大脑中用于HAND治疗的治疗水平。在健康的雌性Sprague-Dawley（SD）大鼠中研究了下一代非核苷类逆转录酶抑制剂rilpivirine（RPV）的大脑分布。提出的研究涉及使用液相色谱-串联质谱（LC-MS / MS）估算血浆和脑匀浆样品中RPV的浓度。基质辅助激光解吸/电离质谱成像（MALDI-MSI）的使用提供了脑组织切片中RPV的区域空间分布。RPV的定位在下丘脑，丘脑和，体中相对较高，下丘脑，丘脑和call体是在HAND期间与神经变性相关的大脑区域（包括大脑皮层）。这项研究表明，RPV具有出色的血脑屏障穿透性。因此，与其他抗逆转录病毒药物联合使用，可以实现更好的中枢神经系统（CNS）预防HAND的保护。这项研究表明，RPV具有出色的血脑屏障穿透性。因此，与其他抗逆转录病毒药物联合使用，可以实现更好的中枢神经系统（CNS）预防HAND的保护。这项研究表明，RPV具有出色的血脑屏障穿透性。因此，与其他抗逆转录病毒药物联合使用，可以实现更好的中枢神经系统（CNS）预防HAND的保护。