阿霉素脂质体的制备及其体外抗肿瘤活性的初步研究

目的:应用超声波分散法制备脂质体阿霉素,并比较脂质体阿霉素与游离性阿霉素抗肿瘤活性。方法:以卵磷脂和胆固醇为原料,将阿霉素包封于脂质体中,采用超声分散法制备脂质体阿霉素,对其在290-700nm范围内进行紫外扫描,用SephedexG-50柱分离脂质体阿霉素并计算其包封率。以昆明种小鼠为载体建立肿瘤模型(S180型肉瘤)和细胞荧光染色法研究脂质体阿霉素的抗肿瘤活性,以ZITA SIZER3000型表面电位与粒度测定仪测定其粒径分布。结果:脂质体阿霉素在480nm处有最大吸收峰值,包封率达91.3%,细胞荧光染色显示,脂质体及游离型阿霉素均对S180细胞有明显的抑制作用。结论:此法制备的脂质体阿霉素包封率高,粒径分布集中,脂质体阿霉素较游离型阿霉素有较强的抗肿瘤活性剂及较低的细胞毒作用,对阿霉素的临床应用有一定的参考价值。

The Preparation of Adriamycin Liposome and the Preliminary Research of itsAnti-tumor Activity in Vitro

Objective:To apply ultrasonic dispersion method to prepare adriamycin liposome, and compare the antitumor activityof adriamycin liposome and free doxorubicin.Methods:As Lecithin and cholesterol as raw materials, the adriamycin was encapsulated inthe liposomes, with in 290-700 nm uv scanning and SephedexG-50 column separation of adriamycin liposome, the coating rate iscalculated. Taking Kunming mice as carrier to establish tumor model and cell fluorescent staining method to study the antitumor activityof the driamycin liposome, making use of ZITA SIZER3000 Surface potential and granularity cryoscope to determine the particle sizedistribution.Results:Adriamycin liposome has maximum absorption peak at 480 nm, and the encapsulation rate was 91.3%, the cellfluorescence staining showed that liposomes and free type of doxorubicin has obvious inhibitory effect on S180 cells.Conclusion:Thismethod of preparation of liposomes doxorubicin coating rate is high and has particle size distribution, the adriamycin liposomedoxorubicin has strong antitumor active agent and low cytotoxic effect, and has certain reference value for the clinical application ofdoxorubicin.