ObjectiveTo establish determination method about capecitabine and oxaliplatin liposomes(Cap-Ox compound liposomes)The Cap and Ox were studied before the prescription,and established methodology certification,the content of Cap and Ox determined the methods determination.The preparation of Cap-Ox compound liposomes studied on,and inspected the character of the galenic pharmacy,the single factor experiment and orthogonal experiment designed the optimization of formulationby.External cytotoxicity test ensured optimum prescription for better curative,the pilot study of antitumous effect.MethodsBy the Sephadex gel micro-column-HPLC to determine the envelopment efficiencies of Cap-Ox into compound liposomes.By the envelopment efficiencies as index,to screening of the best preparation Cap-Ox compound liposomes,For preparation of compound liposomes,the optimization of the formula preparation design through single factor experiment and orthogonal analysis.For investigating the encapsulation efficiency,partical size,form of compound liposomes,measured by TEM and laser particle size analyzer.The research object was human hepatoma cell,though determined by MTT cell toxicity test and western blot,Cap-Ox into compound liposome examine the hepatoma cell of inhibition ratio and the expression of protein of affect the cell apoptosis.The elementary research subserved pesticide effect for the preparation.ResultsRespective built the analysis about the measured content of Cap and Ox,determinate the envelopment efficiency of Cap-Ox compound liposomes by the Sephadex gel micro-column-HPLC.By the film dispersion method,the preparation of liposomes,The consequence of optimized formulation: drug to lipid weight ratio 1:15,the mass ratio of Cap and Ox 10:1,the ratio of phosphatide and cholesterol 3:1 and the concentration of phosphatide 8 g/L,and the average grain diameter of 199.1nm,the average envelopment efficiency of Cap and Ox compound liposomes were 59.8% and 52.6%.The consequence of cell cytotoxicity test in vitro was that in the liposomes of different mass ratio of Cap and Ox,the compound liposomes that the ratio of 15:1 have the best effect that inhibit tumor growth,inhibition of cell growth.the expression of protein of affect the cell apoptosis draw such conclusion that Cap and Ox compound liposomes have better effect then the other dosage form.ConclusionsIn the experiment,Cap and Ox produce into common package in liposomes,Preparation of Cap-Ox compound liposome,For separated the two drugs,changing the ratio of mobile phase and stationary phase,the velocity of flow,the temperature of C18 column and so on,to separate the two drugs,reaching the well shape of peak and the obvious effect of separation,the optimization of formulation by orthogonal analysis,the preparation of Cap-Ox compound liposomes have higher envelopment efficiency,uniform partical size and form.The results of cytotoicity test prove that Cap-Ox compound liposomes can the cancer cell of apoptosis-inducing and have better anti-cancer effect then the other dosage form. |