A novel one-step drug-loading procedure for water-soluble amphiphilic nanocarriers
A novel one-step drug-loading procedure for water-soluble amphiphilic nanocarriers
复制标题
DOI：
10.1023/b:pham.0000029284.40637.69
复制
发表时间：
2004-06-01
影响因子：
3.7
通讯作者：
Leroux, JC
中科院分区：
文献类型：
--
作者：
Fournier, E;Dufresne, MH;Leroux, JC
目的。缺乏水溶性阻碍了许多强效药物的使用。聚合物胶束是一种自组装的纳米载体，具有多种特性，可以被设计成以可控的释放方式溶解、靶向和释放疏水药物。不幸的是，它们的大规模使用受到现有掺入方法的限制，特别是在寻求无菌剂型时。在这篇论文中，我们描述了一种简单、经济和创新的药物装载程序，包括将药物和两亲性二嵌段共聚物溶解在水/叔丁醇混合物中，然后冷冻干燥。我们证明了单分散的20-60纳米大小的载药聚合物胶束在冷冻干燥的蛋糕再水化后直接自发地产生。为了建立原理证明，将两种疏水紫杉烷衍生物溶解在胶束中，并测定了它们的分配系数。这种方法既有效又简单得惊人，可能会引起从事纳米技术和制药科学工作的科学家的极大兴趣。
Purpose. The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited by the incorporation methods available, especially when sterile dosage forms are sought.Methods. In this manuscript, we describe a straightforward, economical, and innovative drug-loading procedure that consists in dissolving both the drug and an amphiphilic diblock copolymer in a water/tert-butanol mixture that is subsequently freeze-dried.Results. We demonstrate that monodisperse 20-60 nm-sized drug-loaded polymeric micelles are produced directly and spontaneously upon rehydration of the freeze-dried cake. To establish the proof-of-principle, two hydrophobic taxane derivatives were solubilized in the micelles, and their partition coefficient was determined.Conclusions. This approach is efficient yet astonishingly simple and may be of great interest for scientists working in nanotechnology and pharmaceutical sciences.