Preparation and characterization of DCA-LTSL / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare decitabine long-circulating thermosensitive liposome(DCA-LTSL), screen and optimize its formulation, and evaluate its properties. METHODS: DCA-LTSL was prepared by modified reverse phase evaporation method, and the encapsulation efficiency was determined by minicolumn centrifugation-HPLC method. The influences of the concentration of PC, the weight ratio of PC to Chol, the weight ratio of DCA to PC and buffer salts were studied. Orthogonal design was adopted to obtain the optimal prescription using encapsulation efficiency as the main index. RESULTS: The best prescription was as follows; the concentration of PC was 5 g · L-1, the weight ratio of PC to Chol was 4 1, the weight ratio of DCA to PC was 40 1 and the pH value of aqueous phase was 7.0.The encapsulation efficiency of DCA-LTSL was (44.50 ± 1.08)% . The Zeta potential was -8.34 mV. The mean diameter of DCA-LTSL was (140.25 ± 2.40)nm. The burst release effectiveness of DCA-LTSL was 42-43°C. CONCLUSION: The formulation of DCA-LTSL has been optimized with excellent in vitro drug release characteristics at the phase-thransition temperature.