水溶性紫杉醇两亲性共聚物纳米胶束研究

聚乙二醇聚己内酯聚乙二醇采用三嵌段共聚物为载体包载紫杉醇形成纳米胶束,胶束具有明显的核壳结构,有效地改善了紫杉醇的水溶性。研究表明,采用蒸发溶剂法、透析法和熔融法制备的胶束对紫杉醇都呈现良好的包封效果,其中,以熔融法制得的胶束粒径最小,分布最窄。文中还考察了蒸发溶剂法实验条件对胶束的影响,发现低沸点有机溶剂有利于获得小粒径胶束,胶束平均粒径随着载药量的提高相应增大。体外释药的结果表明,载药量高的胶束释药率却相对较小。

A new water-soluble nano-micelle formulation of paclitaxel loaded in amphiphilic block copolymer

Tri-block copolymer PEG-PCL-PEG (PECL) was applied as carrier to encapsulate paclitaxel to form nano-micelle with clear core-shell structure, and water solubility of the encapsulated paclitaxel was improved. Solvent evaporation, dialysis and solid dispersion technique were used to prepare the micelle loaded with paclitaxel. It shows that the nano-micelle prepared by solid dispersion technique possesses the smallest average diameter and sharp diameter distribution, and all methods have good encapsulation efficiencies. The effects of different parameters such as temperature, agitating speeds, organic solvents,etc. on the micelle preparations were studied. It indicates that low boiling point of organic solvent is favored for getting smaller diameter micelle, and micelle with high drug loaded content has big diameter. In vitro drug release of PECL micelle loaded with paclitaxel was studied primarily.