Preparation and Characterization of 5-Fluorouracil Long-circulating Liposomes
Objective To prepare 5-Fluorouracil(5-FU)long-circulating liposome modified with polyethylene glycol,optimize the prescription and formulation,and establish the preliminary characterization evaluation.Methods The 5-FU phospholipid long-circulating liposomes were prepared by reverse evaporation method and modified with polyethylene glycol(DSPE-mPEG2000).The effects of the ratio of compound phospholipid,the ratio of phospholipid to cholesterol,the ratio of drug to lipid,the pH value of external water,drug loading temperature and time on the encapsulation efficiency of 5-FU long-circulating liposomes were investigated by single factor test.The encapsulation efficiency was determined by ultraviolet spectrophotometry,and the encapsulation efficiency was taken as the index.The effects of egg yolk lecithin(E80)/hydrogenated Soy Phosphatidylcholine(HSPC)mass ratio,drug-lipid ratio,phosphatidylcholine/cholesterol mass ratio and external aqueous buffer pH on the quality of liposomes were investigated.On this basis,orthogonal design was used to optimize the prescription.The pharmacologic properties of 5-fluorouracil long-circulating liposomes and the sample stability of the liposomes at 4 ℃ for 30 days were investigated.Results The encapsulation efficiency and drug loading of 5-FU long-circulating liposomes prepared by reverse evaporation method were(68.81±0.22)％and(5.47±0.02)％respectively.Electron microscope results and particle size detection showed that the average particle size was about 107 nm,the PDI value was stable below 0.3,and the particle size distribution was uniform and unimodal.At 4 ℃,there was no significant change in the encapsulation efficiency after 3 days,but the encapsulation efficiency decreased by(2.86±0.21)％after 30 days.Conclusion The preparation process of 5-fluorouracil long-circulating liposome modified with polyethylene glycol is simple,feasible and stable.
5-fluorouracilcompound phospholipidlong-circulating liposomeorthogonal test
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