Ooya Tooru, Lee Jaehwi, Park Kinam
School of Materials Science, Japan Advanced Institute of Science and Technology, Tatsunokuchi, Ishikawa 923-1292, Japan.
J Control Release. 2003 Dec 5;93(2):121-7. doi: 10.1016/j.jconrel.2003.07.001.
New methods and pharmaceutical compositions were developed to increase the aqueous solubility of paclitaxel (PTX), a poorly water-soluble drug. Graft and star-shaped graft polymers consisting of poly(ethylene glycol) (PEG400) graft chains increased the PTX solubility in water by three orders of magnitude. Polyglycerol dendrimers (dendriPGs) dissolved in water at high concentrations without significantly increasing the viscosity and, at 80 wt.%, were found to increase the solubility of PTX 10,000-fold. The solubilized PTX was released from graft polymers, star-shaped graft polymers, and the dendriPGs into the surrounding aqueous solution. The release rate was a function of the star shape and the dendrimer generation. The availability of the new graft, star and dendritic polymers having ethylene glycol units should permit development of novel delivery systems for other poorly water-soluble drugs.
人们开发了新的方法和药物组合物，以提高难溶性药物紫杉醇（PTX）的水溶性。由聚乙二醇（PEG400）接枝链组成的接枝和星形接枝聚合物使PTX在水中的溶解度提高了三个数量级。聚甘油树枝状聚合物（dendriPGs）在高浓度下可溶于水，且不会显著增加粘度，在80 wt.%时，可使PTX的溶解度提高10000倍。溶解的PTX从接枝聚合物、星形接枝聚合物和dendriPGs释放到周围的水溶液中。释放速率是星形和树枝状聚合物代数的函数。具有乙二醇单元的新型接枝、星形和树枝状聚合物的可用性应有助于开发其他难溶性药物的新型递送系统。
