Comparative manufacture and cell-based delivery of antiretroviral nanoformulations.
Comparative manufacture and cell-based delivery of antiretroviral nanoformulations.
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DOI：
10.2147/ijn.s27830
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发表时间：
2011
影响因子：
8
通讯作者：
Gendelman HE
中科院分区：
文献类型：
--
作者：
Balkundi S;Nowacek AS;Veerubhotla RS;Chen H;Martinez-Skinner A;Roy U;Mosley RL;Kanmogne G;Liu X;Kabanov AV;Bronich T;McMillan J;Gendelman HE
结晶茚地那韦、利托那韦、阿扎那韦和依非韦伦的纳米制剂是通过湿磨、均质或超声处理与各种赋形剂制造的。使用已建立的单核细胞源性巨噬细胞评分指标系统比较这些制剂的化学、生物、免疫、病毒学和毒理学特性。药物摄取、保留、释放和抗逆转录病毒活性的测量显示了制备方法之间的差异。有趣的是，对于药物细胞靶向和抗逆转录病毒反应，颗粒之间最显着的差异是药物本身。我们认为药物和制剂成分的选择可能最终影响临床效用。
Nanoformulations of crystalline indinavir, ritonavir, atazanavir, and efavirenz were manufactured by wet milling, homogenization or sonication with a variety of excipients. The chemical, biological, immune, virological, and toxicological properties of these formulations were compared using an established monocyte-derived macrophage scoring indicator system. Measurements of drug uptake, retention, release, and antiretroviral activity demonstrated differences amongst preparation methods. Interestingly, for drug cell targeting and antiretroviral responses the most significant difference among the particles was the drug itself. We posit that the choice of drug and formulation composition may ultimately affect clinical utility.