长效福沙那韦脂质纳米颗粒的研制。
Development of an extended action fostemsavir lipid nanoparticle.
机构信息
Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA.
Department of Biochemistry and Molecular Biology, University of Nebraska Medical Center, Omaha, NE, USA.
出版信息
Commun Biol. 2024 Jul 30;7(1):917. doi: 10.1038/s42003-024-06589-5.
An extended action fostemsavir (FTR) lipid nanoparticle (LNP) formulation prevents human immunodeficiency virus type one (HIV-1) infection. This FTR formulation establishes a drug depot in monocyte-derived macrophages that extend the drug's plasma residence time. The LNP's physicochemical properties improve FTR's antiretroviral activities, which are linked to the drug's ability to withstand fluid flow forces and levels of drug cellular internalization. Each is, in measure, dependent on PEGylated lipid composition and flow rate ratios affecting the size, polydispersity, shape, zeta potential, stability, biodistribution, and antiretroviral efficacy. The FTR LNP physicochemical properties enable the drug-particle's extended actions.
一种延长作用的福替拉韦（FTR）脂质纳米颗粒（LNP）制剂可预防人类免疫缺陷病毒 1 型（HIV-1）感染。该 FTR 制剂在单核细胞衍生的巨噬细胞中建立了一个药物储存库，从而延长了药物在血浆中的停留时间。LNP 的物理化学性质提高了 FTR 的抗逆转录病毒活性，这与药物抵抗流体流动力和药物细胞内化水平的能力有关。每种能力在某种程度上都取决于聚乙二醇化脂质组成和影响粒径、多分散性、形状、Zeta 电位、稳定性、生物分布和抗逆转录病毒疗效的流速比。FTR LNP 的物理化学性质使药物颗粒具有延长作用。
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