The objectives of this study were to reduce the cytotoxic effect of nevirapine (NVP) and to enhance its anti-HIV efficacy through mesoporous silica nanoparticles (MSNPs) mediated delivery. MSNPs were synthesized and characterized by various techniques. Confocal microscopy and flow cytometry results exhibited efficient uptake of FITC-conjugated MSNPs in TZM-bl cells. The NVP was loaded within MSNPs, and its anti-HIV1 efficacy was assessed on HIV1 (R5 and X4 variants) infected TZM-bl cells and further confirmed on peripheral blood mononuclear cells (PBMCs). In vitro assessment of the anti-HIV1 potential of NVP and NVP-MSNPs in HIV1 infected TZM-bl cells and PBMCs showed increased efficacy of NVP upon loading within MSNPs with significant increase in therapeutic index. The increased efficacy against HIV1 was accompanied by reduced cytotoxicity to TZM-bl cells and PBMCs. Further, reverse transcriptase (RT) assay confirmed the inhibitory effect on RTase, which is a key enzyme in HIV-1 replication. The present study showed that entrapment of NVP within MSNPs led to an increased efficacy with reduced cytotoxic effect resulting in the enhanced therapeutic index (TI).

这项研究的目的是减少奈韦拉平（NVP）的细胞毒性作用，并通过介孔二氧化硅纳米粒子（MSNPs）介导的递送增强其抗HIV功效。合成了MSNP，并通过各种技术对其进行了表征。共聚焦显微镜和流式细胞术结果显示在TZM-b1细胞中FITC结合的MSNPs被有效吸收。NVP被装载在MSNPs中，并评估了其对HIV1（R5和X4变体）感染的TZM-bl细胞的抗HIV1功效，并在外周血单核细胞（PBMC）上得到进一步证实。体外评估HIV1感染的TZM-b1细胞和PBMC中NVP和NVP-MSNPs的抗HIV1潜力，结果表明，加载到MSNPs中后，NVP的功效增强，治疗指数显着提高。抗HIV1功效的提高伴随着对TZM-bl细胞和PBMC细胞毒性的降低。此外，逆转录酶（RT）分析证实了对RTase的抑制作用，RTase是HIV-1复制中的关键酶。本研究表明，NVP截留在MSNPs中会导致功效增加，细胞毒性作用降低，从而导致治疗指数（TI）增强。