关键词: 多西紫杉醇, 白蛋白微球, 去溶剂化&mdash, 化学交联法

Abstract: Docetaxel (DT), the only derivative of paclitaxel for clinical application in tumor, is mainly used for the treatment of breast cancer, nonsmall-cell lung cancer, oophoroma, etc. Because of its low solubility, organic solvents and solution adjuvants are always added to the preparation. However, organic solvents and solution adjuvants are pungent. Solubility of docetaxel can be increased by the preparation of docetaxel-loaded bovine serum albumin nanoparticles (DT-BSA-NPs) through desolvation-chemical crosslinking method. In this study, the important factors during preparation were tested, and the optimal conditions were obtained according to the optimized data by Design-expert. These data were as follows: the concentration of albumin was 35 mg·mL^-1, the concentration of DT was 1.03 mg·mL^-1, the ratio of ethanol to water was 3∶1, the dripping speed of ethanol was 0.73 mL·min^-1, the stirring time was 12 h, cross-link ratio of glutaraldehyde and BSA was 2∶1. The particle size of the product is 185 nm, and the drug-loading rate is 14.4%. The developed method successfully helped to improve the water-solubility of docetaxel and therefore provided a good foundation for the animal experiments and clinical applications in days to come.

Key words: docetaxel, BSA-NPs, desolvation-chemical crosslinking method