含双疏水侧链聚磷酸酯脂质体膜材的合成

SYNTHESES OF POLYPHOSPHATES CONTAINING TWO LONG HYDROPHOBIC SIDE CHAINS AS LIPOSOME MATERIALS

以季戊四醇二脂肪酸酯和Ｐ，Ｐ二氯磷酸β溴乙酯为单体，通过溶液缩聚反应合成聚磷酸酯，再经季铵化反应得到三种新的含双疏水侧链的磷脂酰胆碱型聚磷酸酯脂质体膜材．采用逆相蒸发法制备脂质体．电镜观察表明，所有聚合物都能形成脂质体，其直径为２～６μｍ．还研究了对抗肿瘤药物５氟脲嘧啶的包封，其包封率为３０％．

Three new amphiphilic polyphosphates containing two long hydrophobic side chains were synthesized by the polycondensation of pentaerythrite di fatty acid esters with β bromoethyl dichorophosphate in benzene,and then by quaterisation with trimethyl amine.The results of IR, 1H NMR spectra and elemental analyses indicate that all the polymers have the expected chemical structures.Average molecular weight of polymers prior to quaterisation was determined by VPO method.The nitrogen content from elemental anyalyses data showed that the polymers containing 46%～49% of quaternary ammonium side chains.All quaternarized polyphosphates were used to prepare liposome by using reverse phase evaporation method.All of them could form large unilamellar liposome.The diameter of liposome is 2～6 μm.Encapsulation ratio of liposome to 5 fluorouracil was also determined.