Fournier Elvire, Dufresne Marie-Hélène, Smith Damon C, Ranger Maxime, Leroux Jean-Christophe
Faculty of Pharmacy, University of Montreal, C.P. 6128, Succ. Centre-Ville, Montreal, Quebec H3C 3J7, Canada.
Pharm Res. 2004 Jun;21(6):962-8. doi: 10.1023/b:pham.0000029284.40637.69.
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.
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.
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.
This approach is efficient yet astonishingly simple and may be of great interest for scientists working in nanotechnology and pharmaceutical sciences.
许多强效药物因缺乏水溶性而限制了其应用。聚合物胶束是具有多种特性的自组装纳米载体，可通过设计使其以控释方式增溶、靶向和释放疏水性药物。不幸的是，其大规模应用受到现有包封方法的限制，尤其是在寻求无菌剂型时。
在本论文中，我们描述了一种直接、经济且创新的载药方法，该方法是将药物和两亲性二嵌段共聚物溶解在水/叔丁醇混合物中，随后进行冷冻干燥。
我们证明，冷冻干燥饼复水后可直接自发产生单分散的20 - 60纳米大小的载药聚合物胶束。为了建立原理验证，将两种疏水性紫杉烷衍生物溶解在胶束中，并测定了它们的分配系数。
这种方法高效且极其简单，可能会引起纳米技术和制药科学领域科学家的极大兴趣。
