聚合脂质体的热敏性研究

Thermo sensitivity of polymeric liposomes

目的：研究获得稳定性好、靶向性强的脂质体。方法：以合成的磷脂酰乙醇胺型聚磷酸酯为膜材，采用ＲＥＶ法制备脂质体。结果：偏光显微镜结果表明，制得的脂质体Ｍ１～Ｍ３为大单层脂质体（ｌａｒｇｅｕｎｉｌａｍｅｌａｒｖｅｓｉｃｌｅｓ，ＬＵＶ）。对５氟尿嘧啶的包封率约为４３％～４５％。热敏试验表明Ｍ１在３９℃～４１℃，Ｍ２在３７℃～３９℃，Ｍ３在３７℃～３９℃，对包封药物有最大泄露率。ＤＳＣ曲线表明，Ｍ２的相变温度ｔｍ为３８５℃，与热敏试验相吻合。结论：合成的聚磷酯酯膜材均能形成良好脂质体，热敏试验和ＤＳＣ曲线证实通过混配可获得较好的热敏脂质体。

OBJECTIVE: To obtain liposomes that exhibit good stability and good targetability. METHODS: All materials (M 1～M 3) could form large unilamellar vesicles (LUV) detected by polarized optical microscope.RESULTS: Encapsulation efficiency of liposome (Ⅱ a-d ) to 5 FU was about 43%～45%. Thermo sensitive test indicated that M 1～M 3 have the largest release rate in 37 ℃～41 ℃. DSC indicated that t m of M 2 is 38.5 ℃, similar to that of thermo sensitive test. CONCLUSIONS: Experimental results showed that these amphiphilic polyphosphates are good materials for preparing liposomes and have good thermo sensitivity.