基于新型酸性自我组装基基的药物递送系统:对N端调制,组装机制和应用的洞察
Yang Guo1, Yang Deng1, Wei Huang2
1Qingdao Institute of Bioenergy and Bioprocess Technology, Chinese Academy of Sciences, No. 189, Songling Road, Qingdao 266101, China; Shandong Energy Institute, Qingdao 266101, China; Qingdao New Energy Shandong Laboratory, No. 189, Songling Road, Qingdao 266101, China; University of Chinese Academy of Sciences, Beijing 100049, China.
这项研究开发了用于口服药物输送的酸稳定基凝. G ((RADA) 4水凝抵抗胃中的降解,并在肠道释放药物,改善胃肠道药物输送.
科学领域:
- 生物材料科学 生物材料科学
- 药物输送系统 药物输送系统
- 体自组装器 自组装器
背景情况:
- 自组装的基凝显示出药物输送的前景.
- 胃肠道应用受到素降解和pH响应不佳的限制.
研究的目的:
- 调查N端残留物如何影响 (RADA) 4的水凝特性.
- 开发耐酸和耐素的水凝,用于口服药物输送.
主要方法:
- 系统地调查X的变种 (X=G/S/A/M/Q/D/C/H).
- 水凝的物理化学特性 (可溶性,自组装,纤维直径,热稳定性) 的表征.
- 评估酸和素耐药性,药物释放动力学 (硫素,胰岛素) 和结构分析 (TEM,冷-SEM).
主要成果:
- 在pH 1.2下,X(RADA) 4种变体 (X=G/S/A/M/Q/D) 形成了pH 1.2的β-sheet纳米纤维水凝,具有不同的纤维直径和热稳定性.
- G ((RADA) 4表现出最佳的产量,抗酸/素,以及适合于口服载体.
- 观察到pH响应的药物释放:在胃pH (2.0) 释放最小,在肠pH (7.2) 释放显著.
结论:
- 酸稳定的G(RADA) 4水凝系统最大限度地减少了胃药物损失.
- 能够针对性地通过肠道输送硫沙和胰岛素等药物.
- 突出了改善胃肠道药物输送平台的巨大潜力.
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