戴单单 陈光辉 徐萍

    [摘要] 目的 以阿霉素为模型药物，制备新型的纳米级醇质体-丙二醇脂质体(A-PL)，并考察其体外抗肿瘤作用。 方法 制备A-PL，并通过透射电镜、激光粒度分析仪、电位测定仪等观察其微观形态、测定粒径和电位。以人肝癌细胞HepG-2为模型细胞株，采用MTT法考察A-PL体外细胞毒性，利用流式细胞仪和倒置荧光显微镜观察HepG-2对A-PL的摄取，采用罗丹明试剂检测细胞的P-糖蛋白(P-gp)功能。 结果 A-PL外观圆整，分散性好，无聚集。平均粒径为150 nm，Zeta电位为-5.78 mV，包封率为83.7%。A-PL的细胞毒性显著高于阿霉素溶液;A-PL能增加细胞对药物的摄取。此外，A-PL更容易进入细胞，且与细胞核有较强的亲和性。A-PL能抑制P-gp的过表达。 结论 本研究制备的A-PL克服了传统脂质体易聚集的缺点，具有稳定、粒径小的优点，具有较好的抗肿瘤效果，作用机制则是主要依赖于A-PL的强内吞作用及泊洛沙姆对药物外排泵的抑制。

    [关键词] 丙二醇脂质体;阿霉素;抗肿瘤;HepG-2

    [中图分类号] R943;R96? ? ? ? ? [文献标识码] A? ? ? ? ? [文章编号] 1673-7210(2019)02(a)-0034-05

    [Abstract] Objective To prepare a novel nano-alcoholic plastid-propylene glycol liposome， namely， adriamycin propanediol liposomes (A-PL) using adriamycin as a model drug and to investigate its anti-tumor effect in vitro. Methods A-PL glycol liposomes were prepared and their microscopic morphology， particle size and potential were observed by transmission electron microscopy， laser particle size analyzer and potentiometer. Human hepatoma cell line HepG-2 was used as the model cell line. The cytotoxicity of A-PL was examined by MTT assay. The uptake of A-PL by HepG-2 was observed by flow cytometry and inverted fluorescence microscopy. The function of P-glycoprotein (P-gp) was detected by rhodamine reagent. Results A-PL had a round appearance ......