Study on Optimization of Preparation and Formulation of Docetaxel-Containing Liposomes

OBJECTIVE To optimize the preparation and formulation of docetaxel-containing liposomes.METHODS Orthogonal design was adopted to screen the preparation and formulation of docetaxel-containing liposomes on the basis of the comprehensive score of the encapsulation efficiency,particle size and stability of liposomes.RESULTS The ideal combination of preparation and formulation were as follows: docetaxel-(lecithin+cholesterol)=1∶20;lecithin-cholesterol=6∶1.The formulation was prepared by thin-film ultrasonic dispersion technique using specified volume of PBS as hydrating medium.The concentration of liposome solution was 0.5 g·L-1.The average encapsulation efficiency of the optimized liposome was(84.4±1.6)%,the average particle size was(147.1±41.1)nm and the Zeta potential was(+2.25±0.2)mV.The docetaxel liposome was quite stable after being stored in refrigerator for 6 months.The sustained release was obtained in vitro.CONCLUSION The thin-film ultrasonic method and the optimized preparation can be used to prepare docetaxel liposome successfully.