用乙烯酸结合剂设计的阴离子脂质:形态偏好,水解稳定性和高药物载荷能力
Anand Kumar Awasthi1, Somnath D Bhagat1, Aditi Banerjee1
1Department of Chemistry, Indian Institute of Science Education and Research (IISER) Bhopal, Bhauri Bhopal Bypass Road, Bhopal, 462066, India.
Chembiochem : a European journal of chemical biology
|July 17, 2023
概括
为了有效的药物输送,合成了新的酸乙脂质 (CALs). 这些脂质形成稳定的囊泡,使高药载荷和有效的细胞传递成为可能,通过聚多巴胺涂层增强生物相容性.
科学领域:
- 生物医学工程 生物医学工程
- 材料科学 是一种材料科学.
- 有机化学 有机化学
背景情况:
- 脂质是生物医学药物输送系统的关键组成部分.
- 开发具有改进性质的新型合成脂质对于先进的药物和基因输送至关重要.
研究的目的:
- 设计,合成和表征一个酸乙脂类 (CALs) 的库.
- 评估CALs的自组装特性和药物载荷能力.
- 评估CALs在增强药物输送应用中的潜力.
主要方法:
- 通过转乙化协议合成CALs.
- 使用NMR和光异构的生物物理表征.
- 用黄素 (Cur) 进行药物加载研究.
- 形成混合脂质聚合物纳米囊与聚多巴胺 (PDA).
主要成果:
- CALs表现出形状刚性和高水解稳定性.
- 一种特定的CAL (CAL1) 形成了凝聚的囊泡聚合物,达到高达196%的重量/重量黄素负载.
- 含有黄素的CAL1配方被证明可以有效地进入哺乳动物细胞.
- 混合纳米囊显示了增强的血红相容性和细胞相容性.
结论:
- 该研究提出了新型CALs的简单合成,具有有希望的自我组装和药物输送能力.
- 在CAL1中,它显示出在制备水性药物 (如黄素) 中具有很高的潜力.
- 混合脂质聚合物纳米囊为药物和基因传递应用提供了更好的生物相容性.
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