具有负自发曲线的脂质降低了癌症药物帕克利塔塞尔在脂质体中的溶解度
Victoria Steffes1,2, Scott MacDonald3, John Crowe3
1Materials Department, University of California, Santa Barbara, California 93106, USA.
bioRxiv : the preprint server for biology
|October 31, 2023
概括
像DOPE和GMO这样的融合性脂质不会改善包素 (PTX) 在阴阳性脂质体中的溶解性. 局部相互作用,而不是膜结构,限制了这些潜在的癌症药物载体中的PTX负载.
科学领域:
- 生物化学 生物化学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 帕克利塔塞尔 (PTX) 是一种疏水性抗癌药物,需要有效的脂基载体来最大限度地减少副作用.
- 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) 和糖单 (GMO) 等脂质已知具有膜融合特性,这表明它们有可能增强药物输送.
结论:
- 当地分子间相互作用,而不是整体脂质膜结构或融合性,主要控制PTX溶解度.
- 由于药物溶解性差,DOPE和GMO是不适合开发有效的脂质载体的组件,用于帕克利塔塞尔的输送.
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