PEG与zwitterions:这些表面装饰如何决定基于脂质的纳米载体的细胞吸收
Daniel Stengel1, Betül Hilal Demirel1, Patrick Knoll1
1Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria.
Journal of colloid and interface science
|May 27, 2023
概括
基于脂质的纳米载体 (NC) 的Zwitterionic表面装饰显著提高了细胞吸收和肠道透,而不是传统的聚乙烯糖醇 (PEG) 涂层的NCs. 这表明zwitterionicNCs是改善细胞内药物递送的有希望的替代品.
科学领域:
- 纳米技术 纳米技术
- 材料科学 材料科学 材料科学
- 生物医学工程 生物医学工程
背景情况:
- 传统的聚乙烯甘醇 (PEG) 涂层脂基纳米载体 (NCs) 在细胞内药物输送方面面临局限性.
- 对NC的表面修改对于优化其生物相互作用和治疗疗效至关重要.
- 兹维特里昂材料比传统的隐形涂层 (如PEG) 有潜在的优势.
研究的目的:
- 评估zwitterionic表面装饰与PEGylation对基于脂质的纳米载体 (NC) 的影响.
- 评估已修改的NCs的细胞吸收,稳定性,细胞毒性和肠道透.
主要方法:
- 基于脂质的纳米载体 (NCs) 用阳离子,中性和阴离子的zwitterionic涂层制备,并与PEGylated NCs进行比较.
- 评估了生物相关液体中的稳定性,与内体模拟膜的相互作用以及细胞相容性.
- 量化了Caco-2和HEK细胞的细胞吸收,以及通过大鼠肠粘膜的ex-vivo透.
主要成果:
- 兹维特和PEGylatedNCs在肠道液体和粘液中显示出类似的稳定性和生物惰性特性.
- 与PEGylated NCs相比,Zwitterionic NCs表现出优异的内体逃生和显著更高的细胞吸收 (高达60倍).
- 菌性NCs表现出微不足道的细胞毒性和增强的肠道透 (高达8.6倍) 的模型药物.
结论:
- 在基于脂质的NC中用zwitterionic表面活性剂取代PEG表面活性剂是增强细胞内药物递送的可行策略.
- 兹威特基纳米载体显示出克服传统PEGylated系统的局限性的巨大潜力.
- 这些发现支持开发zwitterionic纳米载体,以改善口服药物递送应用.
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