脂类型调节蛋白冠状体的组成和脂纳米盘的活体性能
Feng Pan1, Mengyuan Liu1, Guanghui Li1
1School of Pharmacy, Key Laboratory of Smart Drug Delivery, Ministry of Education & Department of Pharmacy, Jing'an District Central Hospital of Shanghai Fudan University, Shanghai 201203, P. R. China.
Molecular pharmaceutics
|April 12, 2024
概括
脂成分影响脂质纳米盘的稳定性和蛋白质相互作用. 基于POPC的纳米盘显示,由于阿波利波蛋白E沉积,大脑分布得到了增强,这为向药物输送提供了潜在的潜力.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术纳米技术
- 药物运输 药物运输 药物运输
背景情况:
- 基于PEGylated脂质的纳米载体在药物输送中至关重要.
- 纳米载体 - 血蛋白相互作用显著影响*体内*命运.
- 了解这些相互作用是纳米载体设计和临床使用的关键.
研究的目的:
- 为了研究脂成分如何影响血清蛋白相互作用,稳定性,和光盘形状的脂质纳米光盘 (sNDs) 的生物分布.
- 探索纳米盘组成和蛋白质冠状形成之间的关系.
- 评估特定纳米盘配方在向药物输送方面的潜力.
主要方法:
- 使用各种脂物制造磁盘形状的脂质纳米磁盘 (sND).
- 在储存和血清中评估sND的稳定性.
- 研究sND-血清蛋白相互作用,包括补充剂激活和阿波利波蛋白吸附.
- 在体内进行的药理动力学和生物分布研究.
主要成果:
- 所有的sND在15天的存储期间都稳定,但血清稳定性有所不同.
- 基于POPG的sND显示出较低的稳定性和快速清除,这是由于补充剂激活.
- 在补充剂激活和血清稳定性之间发现了负相关性.
- 脂成分没有影响逃避加速血液清理.
- 补充沉积与曲线下的面积相反相关.
- 所有的sND都吸附了阿波利波蛋白,POPC-sND显示出更高的阿波利波蛋白E沉积.
结论:
- 脂选择极大地影响了脂质纳米盘的稳定性和血清中的蛋白质相互作用.
- 基于POPG的sND在体内不太稳定,这是由于补体激活.
- 基于POPC的sND显示通过apolipoprotein E增强了大脑的分布,这表明大脑向药物输送的潜力.
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