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揭示了表面聚合药物纳米晶体在有针对性的交付中的潜力
Jakes Udabe1, Sergio Martin-Saldaña1, Yushi Tao2
1POLYMAT, Applied Chemistry Department, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel de Lardizabal 3, 20018 Donostia-San Sebastián, Spain.
ACS applied materials & interfaces
|August 28, 2024
概括
药物纳米晶体 (NCs) 的表面修饰用聚乙烯糖醇 (PEG) 增强了粘膜组织的透和鼻到脑的输送. 这种策略保持了黄素的存在.
科学领域:
- 纳米技术纳米技术
- 材料科学 材料科学 材料科学
- 药品制造 药品制造 药品制造
背景情况:
- 疏水性药物输送与传统纳米载体面临挑战.
- 纳米晶体 (NCs) 具有较高的药物载荷能力,但需要改进准.
- 对NC的表面工程是对增强交付的未经探索的领域.
研究的目的:
- 开发和评估使用聚乙烯糖醇 (PEG) 聚合的表面修饰药物NC.
- 调查PEGylation对NC的特性,准效率和疗效的影响.
- 探索PEGylatedNCs在鼻至脑药物输送方面的潜力.
主要方法:
- 用PEG.合成和表征表面工程的黄素NCs (~200nm) 和PEG.
- 评估粘膜组织透和粘素结合的情况.
- 在体外鼻至脑模型中评估NCs穿越细胞单层的能力.
- 对修改后的NCs的代谢和促炎活性进行分析.
主要成果:
- 用PEG成功地对黄素NC进行表面工程,改变大小和成分.
- 增强的粘膜组织透率 (15μg/cm2) 完全涂层和低交叉连接 (LCS) PEGNCs.
- 观察到LCS PEG涂层NCs的减少粘素结合.
- 在体外鼻至脑模型中,NCs被证明能够穿过紧密的单层.
- 黄素的疗效没有受到表面修改的影响.
结论:
- 将PEG表面聚合到药物NC上是一种可行的策略,可以增强药物输送.
- 基化NCs显示改善了粘膜透和减少了非特异性结合.
- 这种方法有望在不损害药物的有效性的情况下进行有针对性的鼻至大脑输送.
- 进一步优化表面聚合NCs可以导致更有效的治疗方法.
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