在脂质体膜中,两种高度相关的氨酸的释放动力学之间存在巨大的差异:mTHPP和pTHPP
Judith Kuntsche1, Kirishana Rajakulendran1, Hibo Mohamed Takane Sabriye1
1Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark.
Journal of colloid and interface science
|August 12, 2023
概括
疏水性氨酸的微小结构变化显著影响它们从脂质体释放出来. 由于较强的脂质相互作用,meta-THPP的释放速度较慢,影响药物输送策略.
科学领域:
- 脂质双层动态 脂质双层动态
- 药物输送系统是药物输送系统.
- 物理化学 物理化学
背景情况:
- 从脂质体中释放的疏水性化合物取决于药物的物理化学特性.
- 轻微的结构变化可以影响药物分区和释放动力学.
研究的目的:
- 调查甲型和甲型THPP中的微妙结构差异如何影响它们的分割和从脂质体释放.
- 阐明了差异释放行为背后的分子机制.
主要方法:
- 不对称的流场流量分成 (AF4) 用于分离捐赠和接受颗粒.
- 逆相高性能液态染色学 (RP-HPLC) 用于分区分析.
- 分子动力学 (MD) 模拟用于深入的膜相互作用研究.
主要成果:
- 尽管存在微小的结构差异,但meta-THPP具有更强的疏水性,释放速度比para-THPP慢.
- MD模拟显示meta-THPP与脂质头组形成更强的键,并在双层中嵌入更深.
- 与para-THPP相比,meta-THPP表现出与脂质尾巴更加平行的方向.
结论:
- 类OH组在氨酸中的位置显著改变了它们的脂质体释放动力学.
- 增强的水性和特异性脂质相互作用的meta-THPP导致释放速度较慢.
- 这些发现为设计具有可控释放特征的脂质体药物递送系统提供了洞察力.
更多相关视频
08:49Fluorescence-Based Measurements of Phosphatidylserine/Phosphatidylinositol 4-Phosphate Exchange Between Membranes
Published on: March 14, 2021
4.1K
09:51One Minute, Sub-One-Watt Photothermal Tumor Ablation Using Porphysomes, Intrinsic Multifunctional Nanovesicles
Published on: September 17, 2013
10.9K
相关概念视频
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.5K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.5K
Protein Diffusion in the Membrane
4.4K
Proteins show rotational as well as lateral diffusion across the membrane. The lateral diffusion of proteins was confirmed through the cell fusion experiment where mouse and human cells were fused, resulting in hybrid cells. When the human and mouse cells fused, the specific membrane proteins on human and mouse cells were marked with the red and green-fluorescent markers, respectively. Initially, the red and green fluorescence was located on the respective hemisphere of the cell. As time...
4.4K
