Catanionic vesicles from an amphiphilic prodrug molecule: a new concept for drug delivery systems
Catanionic vesicles from an amphiphilic prodrug molecule: a new concept for drug delivery systems
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来自两亲性前药分子的阴离子囊泡：药物递送系统的新概念
DOI：
10.1039/c2ra20653f
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发表时间：
2012-01-01
期刊：
影响因子：
3.9
通讯作者：
Li, Zhonghao
中科院分区：
文献类型：
--
作者：
Jiang, Yue;Luan, Yuxia;Li, Zhonghao
阳离子 - 阴离子混合囊泡在药物应用方面主要存在毒性和包封率低的问题。为了尽量降低表面活性剂的毒性，提高载药量，同时减少繁琐的化学合成需求，我们使用油酸作为生物相容性表面活性剂，它与选定的药物分子（氨氯地平）反应生成一种两亲性前药分子，用于直接制备阳离子 - 阴离子混合囊泡。前药分子可通过氨氯地平和油酸分子之间的质子转移轻松获得。利用傅里叶变换红外光谱（FTIR）、氢 - 1 - 核磁共振（H - 1 - NMR）、差示扫描量热法（DSC）、表面张力测量、透射电子显微镜（TEM）、动态光散射（DLS）、电导率和ζ电位（zeta）对前药分子及其在水溶液中的聚集行为进行了表征。结果表明，两亲性前药分子分散在水溶液中时很容易形成囊泡。特别是，所制备的阳离子 - 阴离子混合囊泡的药物释放行为表现出优异的缓释特性，这表明它们在新设计的药物递送系统中具有良好的应用前景。
Toxicity and low entrapment efficiency are the main problems for pharmaceutical applications of catanionic vesicles. In order to minimize surfactant toxicity, increase the drug loading content and simultaneously reduce the need for tedious chemical synthesis, we use oleic acid as the biocompatible surfactant, which reacts with the selected drug molecules (amlodipine) to produce an amphiphilic prodrug molecule for the straightforward fabrication of catanionic vesicles. The prodrug molecules are easily obtained by proton transfer between amlodipine and oleic acid molecules. The characterization of prodrug molecules and their aggregation behaviours in aqueous solutions are investigated by using Fourier transform infrared spectrophotometry (FTIR), 1H-nuclear magnetic resonance (1H-NMR), differential scanning calorimetry (DSC), surface tension measurement, transmission electron microscopy (TEM), dynamic light scattering (DLS), conductivity and zeta potential (ζ). The results demonstrate that vesicles could be easily formed with the prodrug amphiphilic molecules dispersed in aqueous solutions. Particularly, the drug release behaviour of the as-prepared catanionic vesicles exhibits excellent sustained drug release properties, which demonstrates their promising application in the newly designed drug delivery system.