文獻：優化藥物輸送：通過 31P 和 2H NMR 光譜表征 DLin-KC2-DMA/二硬脂酰磷脂酰絲氨酸

鏈接：https://summit.sfu.ca/item/15257

作者：林賽·T·約翰遜張迪周克進李桑明劉帥肖恩·A·迪利亞德盧卡斯·法比亞克蘇曼塔·查特吉林玉軒丹尼爾·J·西格瓦特*

節選：

脂質納米顆粒 (LNP) 用于通過內吞作用和隨后的內體釋放將 siRNA 遞送至肝細胞。由于 99% 的 LNP 是通過內吞作用被細胞吸收的，因此只有 1% 的 siRNA 真正被釋放到細胞質中。為了提高 LNP 與內體膜結合及其破壞的有效性，采用 2H 和 31P NMR 光譜法表征了由 1:1 摩爾比的陰離子脂質 1,2-二硬脂酰(d70)-sn-甘油-3-[磷酸-L-絲氨酸] (DSPS-d70) 和陽離子脂質 DLin-KC2-DMA 組成的模型體系的生物物理特性。結果表明，該模型體系從雙層相向倒六邊形相 (HII) 的相變受溫度、pH 值和鹽濃度的影響。獲得了序參數分布圖，揭示了DSPS-d70在雙層膜和HII相中酰基鏈運動的程度。這些結果有助于為計算模擬以及*終優化的LNP設計提供參考。

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.

西安齊岳生物提供相關產品：

DSPE-NHS

DSTAP (18:0)

DSPE-PEG-SH

Cy3-DPPE

DSPE-PEG-HA

DPPE-PEG-N3

Cy7-DOPE

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