从热敏脂质体中迅速释放多克索鲁比――泄漏与卸载的贡献
Henriette Hummler1, Maximilian Regenold2, Christine Allen2
1Institute of Pharmaceutical Sciences, University of Freiburg, Freiburg D-97104, Germany.
The journal of physical chemistry. B
|July 10, 2025
概括
从热敏脂质体中释放药物是通过泄漏和卸载发生的. 卸载对过渡温度以上的多克索鲁素快速释放有显著的贡献,但在过渡温度以下的脂质透性受到限制.
科学领域:
- 生物医学工程 生物医学工程
- 药品制造 药品制造 药品制造
- 药物运输 药物运输 药物运输
背景情况:
- 脂质体是药物输送的关键纳米载体.
- 远程加载可以提高药物封装效率.
- 了解药物释放机制对于优化脂质体配方至关重要.
研究的目的:
- 区分和量化含脂热敏脂质体 (LTSL) 中的药物泄漏和卸载贡献.
- 调查多克索鲁比从LTSL释放的机制,跨越它们的相位过渡温度.
- 阐明pH值和温度在药物释放动力学上的作用.
主要方法:
- 使用pH梯度远程加载制备了多克索鲁比辛载荷的LTSL.
- 药物释放在物理 (pH 7.4) 和酸性 (pH 5.0) 条件下的缓冲器中被测量.
- 在脂质相转换温度 (≈41°C) 以上和以下分析了释放概况.
主要成果:
- 在过渡温度以上,卸载约占30秒内快速释放多克索鲁比辛的30%.
- 在过渡温度以下,药物释放量减少,尽管部分pH梯度崩,但卸载量有限.
- 脂质双层的凝阶段显著限制了多克索鲁比辛的透,即使是在其脱质的形式.
结论:
- 泄漏和卸载都有助于从LTSL释放多克索鲁.
- 卸载是一个重要的,取决于温度的释放途径,主要发生在脂质相过渡以上.
- 脂质相和pH条件极大地影响每个释放机制的贡献,影响药物递送概况.
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