Intracellular delivery of saquinavir in biodegradable polymeric nanoparticles for HIV/AIDS
Intracellular delivery of saquinavir in biodegradable polymeric nanoparticles for HIV/AIDS
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DOI：
10.1007/s11095-006-9101-7
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发表时间：
2006-11-01
影响因子：
3.7
通讯作者：
Amiji, Mansoor M.
中科院分区：
文献类型：
--
作者：
Shah, Lipa K.;Amiji, Mansoor M.
目的：本研究的目的是开发聚环氧乙烷修饰的聚己内酯（PEO-PCL）纳米粒系统作为沙奎那韦，抗HIV蛋白酶抑制剂的细胞内delivery vehicle.Materials和方法：沙奎那韦的PEO-PCL纳米粒通过溶剂置换过程制备。所形成的纳米颗粒的大小，表面电荷，和表面存在的PEO链进行了表征。在THP-1人单核细胞/巨噬细胞（Mo/Mac）细胞系中检查纳米颗粒的细胞摄取和分布。细胞内沙奎那韦浓度测定作为剂量和持续时间的函数incubation.Results：聚氧化乙烯-聚己内酯纳米粒子具有光滑的表面和球形的形状，并表现出相对均匀的粒径分布，平均粒径约为200 nm。PEO链的表面存在下，证实了增加的-C-O-（醚）签名的C1 s光谱的电子光谱化学分析。在THP-1细胞中观察到罗丹明-123包封的PEO-PCL纳米颗粒的快速细胞摄取。胞内沙奎那韦浓度时，在纳米颗粒制剂管理显着高于从水solution.Conclusions：这项研究表明，PEO-PCL纳米粒子提供了一个通用的平台，沙奎那韦的封装和随后的细胞内交付在Mo/Mac细胞。
Purpose: This study aims at developing poly(ethylene oxide)-modified poly(epsilon-caprolactone) (PEO-PCL) nanoparticulate system as an intracellular delivery vehicle for saquinavir, an anti-HIV protease inhibitor.Materials and Methods: Saquinavir-loaded PEO-PCL nanoparticles were prepared by a solvent displacement process. The formed nanoparticles were characterized for size, surface charge, and surface presence of PEO chains. Cellular uptake and distribution of the nanoparticle was examined in THP-1 human monocyte/macrophage (Mo/Mac) cell line. Intracellular saquinavir concentrations were measured as a function of dose and duration of incubation.Results: The PEO-PCL nanoparticles had a smooth surface and spherical shape and showed a relatively uniform size distribution with a mean particle diameter of approximately 200 nm. The surface presence of PEO chains was confirmed by an increase in the -C-O-(ether) signature of the C1s spectra in electron spectroscopy for chemical analysis. Rapid cellular uptake of rhodamine-123 encapsulated PEO-PCL nanoparticles was observed in THP-1 cells. Intracellular saquinavir concentrations when administered in the nanoparticle formulation were significantly higher than from aqueous solution.Conclusions: This study shows that PEO-PCL nanoparticles provide a versatile platform for encapsulation of saquinavir and subsequent intracellular delivery in Mo/Mac cells.