Abstract: Objective To prepare the folic acid coupled nano-paclitaxel drug for targeted tumor therapy. Methods Nano-paclitaxel was prepared by polycarbonate membrane dispersion-extrusion. The method of ultrasonic emulsification-solvent evaporation was adopted to prepare DSPE-PEG2000-FA micelle. Co-incubation method was used to prepare DSPE-PEG2000-FA modified folic acid coupling nano-paclitaxel. The mean diameter of folic acid coupling nano-paclitaxel drugs and the encapsulation efficiency were determined by zetasizer and elution curve of drug. Results Compared with the diameter of nano-paclitaxel particle［(121.6±12.7) nm］and polydispersity index (PDI) (0.262±0.031), the mean diameter of folic acid coupling nano-paclitaxel drugs ［(140.5±10.3) nm］ and PDI (0.263±0.061) were slightly larger, but the difference was not statistically significant (t=2.013; P=0.114). In contrast to the encapsulation efficiency of the crude drugs (nano-paclitaxel drugs) 99%, the encapsulation efficiency of folic acid coupling nano-paclitaxel drugs was as high as 97% with no significant decline, which ensures purity and effectiveness of the drugs. Conclusion The novel formulation of FR-targeted folic acid coupling nano-paclitaxel is reported. This formulation has good drug loading properties, drug encapsulation efficiency, and exhibits excellent colloidal stability.

Key words: folic acid monomethoxy-polyethylene glycol 2000-distearoyl phosphatidylethanolamine, nano-liposomes, paclitaxel, particle size, encapsulation