在脂质体中绘制柏柏林分布:药物-脂相互作用在局部化和释放中的作用
Namrata Dhakal1, Yan Cao2, Flavio Costa3
1Department of Pharmacy, Faculty of Science, National University of Singapore, 4 Science Drive 2, 117544, Singapore.
International journal of pharmaceutics
|August 26, 2025
概括
药物在脂质体内的局部化显著影响释放率. 在脂质体中含有较高度的带电脂质会加速柏柏林的释放,这是由于表面吸附而不是更快的膜透.
科学领域:
- 纳米技术
- 材料科学
- 生物物理
背景情况:
- 脂质体是有效的药物输送纳米载体.
- 了解脂质体内的药物定位对于控制药物释放动力学至关重要,特别是对于两性药物.
- 膜组成和药物脂质相互作用对脂体内药物分布和随后释放的影响尚不完全理解.
研究的目的:
- 调查药物局部化如何受脂质体膜组成和加载程序的影响,影响两性药物Berberine的释放动力学.
- 阐明静电相互作用和膜架构在控制柏柏林体内分布和释放行为的作用.
主要方法:
- 使用双离心法制备具有不同含量的1,2-二甲基糖-3-醇 (DPPC) 和1,2-二甲基糖-3-糖醇 (DPPG) 的脂质体.
- 用光谱和热量测量分析来确定脂质体内的柏柏林定位.
- 在体外释放药物的研究.
- 分析脂质体膜结构和药物脂质相互作用的分子动力学模拟.
主要成果:
- 柏柏林主要局限于DPPC脂质体的水性核心.
- 加入DPPG导致柏柏林分离到脂质双层和表面吸附.
- 由于静电相互作用,较高的DPPG含量导致了较宽松的双层包装,每脂质面积增加,双层厚度减少.
- 具有较高DPPG含量的脂质体表现出快速的柏柏林释放,这归因于表面定位.
- 降低药物负载有利于将药物分离到内部双层,减缓释放速度.
结论:
- 在脂质体内药物定位是释放贝尔贝林等两性化合物的动力学的关键决定因素.
- 脂质体膜组成,静电相互作用和加载程序显著影响药物的分发和释放.
- 这项研究为设计针对特定药物的先进脂肪体药物递送系统提供了机理性见解.
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