化α-cyclopodextrin:可能是最小的药物载体,提供增强的细胞吸收和内体细胞逃逸
Özlem Kaplan1, Martyna Truszkowska2, Gergely Kali2
1Department of Genetics and Bioengineering, Rafet Kayış Faculty of Engineering, Alanya Alaaddin Keykubat University, 07400 Antalya, Turkey; Department of Molecular Biology and Genetics, Faculty of Science, Istanbul University, 34134 Istanbul, Turkey.
Carbohydrate polymers
|June 15, 2023
概括
化α-环极 (α-CD-SH) 显著增强细胞吸收药物有效载荷,改善向细胞的输送. 这种修改后的环极素也促进了内体逃生,显示出作为药物输送载体的希望.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 阿尔法-环极德 (α-CD) 是一种周期性寡糖,具有药物输送潜力.
- 用醇组 (α-CD-SH) 修改α-CD可能会增强其细胞相互作用和有效载荷传递.
- 有效的细胞吸收和内体逃逸对于有效的细胞内药物递送至关重要.
研究的目的:
- 为了合成和表征化α-环极素 (α-CD-SH).
- 评估α-CD-SH对细胞吸收制药有效载荷的影响.
- 为了研究α-CD-SH.的内体体逃生能力.
主要方法:
- 使用 pentasulfide 的 α-CD-SH 的合成.
- 使用FT-IR,1H NMR,DSC和PXRD进行表征.
- 对Caco-2,HEK 293和MC3T3细胞的细胞毒性评估.
- 通过流细胞计和共聚焦显微镜对Dilauryl光素 (DLF) 和素-6 (Cou) 的细胞吸收分析.
- 使用共聚焦显微镜和血液溶解试验进行内体逃生评估.
主要成果:
- α-CD-SH在3小时内没有表现出细胞毒性,但在24小时内表现出剂量依赖的细胞毒性.
- 与原生α-CD相比,α-CD-SH对DLF和Cou的细胞吸收分别增加了20倍和11倍.
- α-CD-SH 证明了促进内体逃逸的能力.
结论:
- 化α-环极 (α-CD-SH) 是增强药物输送的有希望的载体.
- 与原生α-CD.SH相比,α-CD-SH显著改善了细胞对有效载荷的吸收.
- α-CD-SH的内体体逃逸特性进一步支持其在细胞质药物递送中的潜力.
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