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两性杯[8]芳烃为基础的药物输送的 pH 触发型复合物。

Amphoteric calix[8]arene-based complex for pH-triggered drug delivery.

机构信息

Department of Chemical Engineering, University of New Brunswick, Fredericton, New Brunswick, Canada.

出版信息

Colloids Surf B Biointerfaces. 2013 Jan 1;101:55-60. doi: 10.1016/j.colsurfb.2012.06.022. Epub 2012 Jun 29.

DOI:10.1016/j.colsurfb.2012.06.022
PMID:22796772
Abstract

Amphoteric calix[8]arene with negatively charged upper rim and positively charged lower rim was synthesized based on water-soluble p-sulfonato-calix[8]arene. The pH-sensitive amphoteric calix[8]arenes exhibit not only a good hydrophobic drug loading capacity but also a pH-triggered drug releasing behavior. The in vitro release studies demonstrated that release of ciprofloxacin from amphoteric calix[8]arene complexes was highly pH-sensitive. More efficient drug release was observed at mildly acidic pH 5.0 and basic pH 8.5 compared to physiological pH. The amphoteric calix[8]arene complexes hold out great promise of being pH-sensitive drug carrier.

摘要

基于水溶性对磺酸钠杯[8]芳烃合成了具有带负电荷的上边缘和带正电荷的下边缘的两性杯[8]芳烃。这种对 pH 值敏感的两性杯[8]芳烃不仅表现出良好的疏水性药物负载能力,而且还表现出 pH 值触发的药物释放行为。体外释放研究表明,两性杯[8]芳烃配合物中环丙沙星的释放对 pH 值高度敏感。与生理 pH 值相比,在略酸性 pH 值 5.0 和碱性 pH 值 8.5 下观察到更有效的药物释放。两性杯[8]芳烃配合物有望成为 pH 值敏感的药物载体。

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