OBJECTIVE To prepare prodrug 5′-palmitoyl-5- fluorouridine (5-FURP) liposome and to evalutate its toxicity in vitro. METHODS The orthogonal design was used to screen the optimal formation and preparation process.The 5-FURP liposome was prepared by the reverse-phase evaporation vesicles(REV),and its encapsulation efficiency and physicochemical property was determined. The cytotoxicity of 5-FURP liposome was investigated by human breast cancer of MCF-7cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line. RESULTS encapsulation efficiency of the 5-FURP liposome was 94.35%. The stability of 5-FURP liposome was valuated with the entrapment efficiency and the change of EPC value in 4,25 ℃ for 1 month. The results showed that the 5-FURP liposome stored in 4 ℃ would keep stable. The results of cell toxicity in vitro showed that the liposomes encapsulated with 5-FURP inhibited human breast cancer of MCF-7 cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line was higher than that of the free drug.The IC50 of 5-FURP liposome was higher(5.0,3.4,2.6 times) for the MCF-7,CNE-1,HEP-2 than for free 5-FUR. CONCLUSION 5-FURP was encapsulated in liposomes can inhance corpuscular uptake and promote therapeutic effect of medicine.
WU Mei-chun;ZHU Li;ZHO Yi;PN Li-jun;WNG Chi.
Study on Preparation of 5′-Palmitoyl-5-Fluorouridine Liposome and Its Cell Toxicity [J]. Chinese Pharmaceutical Journal, 2009, 44(07): 520-523
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