文献：优化药物输送：通过 31P 和 2H NMR 光谱表征 DLin-KC2-DMA/二硬脂酰磷脂酰丝氨酸

链接：https://summit.sfu.ca/item/15257

作者：林赛·T·约翰逊张迪周克进李桑明刘帅肖恩·A·迪利亚德卢卡斯·法比亚克苏曼塔·查特吉林玉轩丹尼尔·J·西格瓦特*

节选：

脂质纳米颗粒 (LNP) 用于通过内吞作用和随后的内体释放将 siRNA 递送至肝细胞。由于 99% 的 LNP 是通过内吞作用被细胞吸收的，因此只有 1% 的 siRNA 真正被释放到细胞质中。为了提高 LNP 与内体膜结合及其破坏的有效性，采用 2H 和 31P NMR 光谱法表征了由 1:1 摩尔比的阴离子脂质 1,2-二硬脂酰(d70)-sn-甘油-3-[磷酸-L-丝氨酸] (DSPS-d70) 和阳离子脂质 DLin-KC2-DMA 组成的模型体系的生物物理特性。结果表明，该模型体系从双层相向倒六边形相 (HII) 的相变受温度、pH 值和盐浓度的影响。获得了序参数分布图，揭示了DSPS-d70在双层膜和HII相中酰基链运动的程度。这些结果有助于为计算模拟以及*终优化的LNP设计提供参考。

Lipid nanoparticles (LNPs) are used to deliver siRNA to hepatocytes via endocytosis and subsequent endosomal release. With 99% of the LNPs taken up by the cell via endocytosis, only 1% of the siRNA is actually released into the cell cytosol. To improve the effectiveness of LNPs association with and disruption of endosomal membranes, the biophysical properties of a model system composed of 1:1 molar ratio of anionic lipid 1,2-distearoyl(d70)-sn-glycero-3-[phospho-L-serine] (DSPS-d70) and the cationic lipid DLin-KC2-DMA are characterized by 2H and 31P NMR spectroscopy. The bilayer to inverted hexagonal (HII) phase transition of the model system was shown to be influenced by temperature, pH and salt concentration. The order parameter profiles are obtained, revealing the extent of acyl chain movement of DSPS-d70 in bilayer and HII phases. The results help provide insights into computational simulation and eventually optimized LNPs design.

西安齐岳生物提供相关产品：

DSPE-NHS

DSTAP (18:0)

DSPE-PEG-SH

Cy3-DPPE

DSPE-PEG-HA

DPPE-PEG-N3

Cy7-DOPE

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