摘要
以4-二甲氨基吡啶(DMAP)和二环己基碳二亚胺(DCC)作催化剂和缩合剂,合成聚乙二醇-共轭亚油酸(PEG-CLA)聚合物;以PEG-CLA为载体,采用透析法制备了紫杉醇聚合物胶束给药系统;利用动态光散射法(DLS)、透射电镜(TEM)、X-射线光电能谱(XPS)表征了紫杉醇胶束的粒径与粒径分布、形貌以及表面组分特性,分别在pH值为7.4的磷酸盐缓冲溶液(PBS)和1 mol/L水杨酸钠溶液中进行了紫杉醇胶束的体外药物释放试验。研究结果表明,所制备的紫杉醇胶束外形大致呈球状,粒径在100 nm左右,且粒径分布较窄。X-射线光电能谱显示,胶束表面没有吸附紫杉醇。在体外药物释放实验中,发现水杨酸钠对紫杉醇的释放起促进作用。
Poly(ethylene glycol) ( PEG)-conjugated linoleic acid (CLA) (PEG-CLA) polymeric conjugate was synthesized using 4-dimethylaminopyridine (DMAP) and dicyclohexycarbodiimide ( DCC ) as catalyst and coupling agent, respectively. PEG-CLA polymer was employed as carder, the paclitaxel-loaded micelles were prepared by dialysis method. The size and size distribution, the structure and the surface chemistry of micelles were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM) and X-ray photoelectron spectroscopy (XPS), respectively. The in vitro release profiles of paclitaxel from polymeric micelles were investigated in pH7.4 phosphate buffer solution (PBS) and 1 mol/L sodium salicylate medium The results show that the paclitaxel-loaded micelles have spherical shapes,particle size of 100 nm and narrow size distribution. XPS indicates that the drug is not absorbed on the micelles surface and sodium salicylate medium can accelerate the release rate of paclitaxel from polymeric micelles.
出处
《化学工业与工程》
CAS
2007年第1期24-27,共4页
Chemical Industry and Engineering
关键词
紫杉醇
聚合物胶束
水杨酸钠
paclitaxel
polymeric micelle
sodium salicylate