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首页> 外文OA文献 >Self-assembled biotransesterified cyclodextrins as potential Artemisinin nanocarriers. II: In vitro behavior toward the immune system and in vivo biodistribution assessment of unloaded nanoparticles.
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Self-assembled biotransesterified cyclodextrins as potential Artemisinin nanocarriers. II: In vitro behavior toward the immune system and in vivo biodistribution assessment of unloaded nanoparticles.

机译：自组装生物酯化的环糊精作为潜在的青蒿素纳米载体。 II：免疫系统的体外行为和未负载纳米颗粒的体内生物分布评估。

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In a previous study, we reported on the formulation of Artemisinin-loaded surface-decorated nanoparticles (nanospheres and nanoreservoirs) by co-nanoprecipitation of PEG derivatives (PEG1500 and PEG4000-stearate, polysorbate 80) and biosynthesized γ-CD fatty esters. In the present study, the co-nanoprecipitation was extended to the use of a PEGylated phospholipid, namely DMPE-PEG2000. As our goal was to prepare long-circulating nanocarriers for further systemic delivery of Artemisinin (ART), here, we have investigated, on the one hand, the in vitro behavior of these surface-modified γ-CD-C10 particles toward the immune system (complement activation and macrophage uptake assays) and, on the other hand, their biodistribution features in mice. These experiments showed that the in vitro plasma protein adsorption and phagocytosis by macrophage cells triggered by γ-CD-C10 nanoparticles were significantly reduced when their surface was decorated with amphiphilic PEGylated molecules, in particular PEG1500-stearate, DMPE-mPEG2000 or polysorbate 80. The prolonged blood circulation time assessed by fluorescence imaging was demonstrated for unloaded γ-CD-C10-based nanospheres and nanoreservoir particles containing DMPE-PEG2000 and polysorbate80, respectively. These nanoparticles also proved to be non-hemolytic at the concentration range used in vivo. Within the limits of the conducted experiments, the co-nanoprecipitation technique may be considered as an alternative for surface modification of amphiphilic CD-based drug delivery systems and may be applied to the systemic delivery of ART.
机译：在先前的研究中，我们报告了通过共纳米沉淀PEG衍生物（PEG1500和PEG4000-硬脂酸酯，聚山梨酸酯80）和生物合成的γ-CD脂肪酸酯，制备负载青蒿素的表面修饰纳米颗粒（纳米球和纳米储液）的方法。在本研究中，共纳米沉淀扩展到使用聚乙二醇化磷脂，即DMPE-PEG2000。由于我们的目标是制备长循环的纳米载体以进一步青蒿素（ART）进行全身递送，因此，我们一方面研究了这些表面修饰的γ-CD-C10颗粒对免疫系统的体外行为（补体激活和巨噬细胞摄取测定），以及它们在小鼠中的生物分布特征。这些实验表明，当用两亲性PEG化分子，特别是PEG1500-硬脂酸酯，DMPE-mPEG2000或聚山梨酯80装饰时，由γ-CD-C10纳米粒子触发的巨噬细胞体外血浆蛋白的吸附和吞噬作用显着降低。分别通过空载的基于γ-CD-C10的纳米球和含有DMPE-PEG2000和聚山梨酯80的纳米储库颗粒，证实了通过荧光成像评估的延长的血液循环时间。这些纳米颗粒在体内使用的浓度范围内也被证明是非溶血的。在所进行实验的范围内，共纳沉淀技术可被视为两亲CD基药物递送系统表面修饰的替代方法，并可应用于ART的系统递送。

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