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本研究的目的是将α-维生素E琥珀酸酯的偶联物Tat-TOS与磷脂酶D抑制剂FIPI以及抗肿瘤药阿霉素共同包载于脂质体递送系统中,用于抗肿瘤转移.首先采用固相合成法合成了Tat-TOS,并对其进行结构确证,用诱导凋亡法考察了游离Tat-TOS和Tat-脂质体的体外诱导细胞凋亡的能力,并评价了表面修饰了Tat-TOS脂质体的肺部靶向特性,采用薄膜分散法结合pH梯度法与后插入法制备了修饰有Tat-TOS的载FIPI和阿霉素的多组分脂质体,并进行理化性质测定,最后评价了细胞对该制剂的体外摄取能力.研究结果表明,所制备脂质体具备粒径分布均一,粒径小的特点,FIPI和DOX的包封率均超过85％,无论是游离还是脂质体包载的Tat-TOS均能显著提高诱导肿瘤细胞凋亡的能力,表面修饰了Tat-TOS的脂质体具有明显聚集于健康肺组织和肿瘤转移肺组织,多组分脂质体具有最强的细胞摄取能力,预示该脂质体制剂具有更强的体外抗转移功效.“,”In the present study,we aimed to co-load the α-TOS conjugate Tat-TOS with the phospholipase D inhibitor FIPI and the antitumor drug doxorubicin (DOX) in a liposome delivery system for antitumor metastasis.Firstly,Tat-TOS was synthesized by solid-phase synthesis,and its structure was confirmed.The ability of free and liposomal Tat-TOS to induce apoptosis in vitro was evaluated by flow cytometry.Biodistribution of Tat-TOS-loaded liposomes was investigated by a molecular imaging system.Multi-component-loaded liposomes modified with Tat-TOS containing FIPI and DOX was prepared by thin film dispersion method in combination with pH gradient method and post-insertion method.Physicochemical properties were determined,and the in vitro uptake ability of the formulations was evaluated.The results showed that the prepared liposomes were characterized by a uniform particle size distribution and small particle size.The encapsulation efficiency of FIPI and DOX exceeded 85％.Both free and liposomal Tat-TOS significantly improved the activity of inducing apoptosis of tumor cells.The liposomes modified with Tat-TOS were apparently accumulated in normal lung tissue and tumor metastasized lung.Multi-component-loaded liposomes exhibited the strongest cell uptake capacity,suggesting a stronger anti-metastatic effect and anti-tumor activity in vivo.